Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
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Bonds
H don H acc LogP Smiles
CHEMBL144397 5ht1b_human Human No 10.1 EC50 = 0.1 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
506 14 6 6 1.7 NCCc1c[nH]c2ccc(OCC(=O)NCCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12
CHEMBL342323 5ht1b_human Human No 10.0 EC50 = 0.1 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
828 25 6 8 7.2 NCCc1c[nH]c2ccc(OCCCCCCNS(=O)(=O)c3ccc(-c4ccc(S(=O)(=O)NCCCCCCOc5ccc6[nH]cc(CCN)c6c5)cc4)cc3)cc12
CHEMBL144128 5ht1b_human Human No 9.7 EC50 = 0.2 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
490 12 4 6 2.7 NCCc1c[nH]c2ccc(OCCN3CCN(CCOc4ccc5[nH]cc(CCN)c5c4)CC3)cc12
CHEMBL147851 5ht1b_human Human No 9.7 EC50 = 0.2 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
504 11 4 6 2.3 NCCc1c[nH]c2ccc(OCCN3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12
CHEMBL357830 5ht1b_human Human No 9.6 EC50 = 0.3 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
600 11 4 6 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCC(C4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)CC3)cc12
CHEMBL146720 5ht1b_human Human No 9.6 EC50 = 0.3 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
518 10 4 6 1.8 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12
CHEMBL356277 5ht1b_human Human No 9.5 EC50 = 0.3 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
540 12 6 6 3.7 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(NC(=O)COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12
CHEMBL357478 5ht1b_human Human No 9.4 EC50 = 0.4 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
609 12 5 7 3.4 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(N4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)cc3)cc12
CHEMBL147901 5ht1b_human Human No 9.4 EC50 = 0.4 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
435 11 5 5 2.2 NCCc1c[nH]c2ccc(OCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12
CHEMBL158941 5ht1b_human Human No 9.2 EC50 = 0.6 nM Funct
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
692 16 2 6 4.8 CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N(C)Cc3ccc(CN(C)S(=O)(=O)Cc4ccc5[nH]cc(CCN(C)C)c5c4)cc3)cc12
CHEMBL424128 5ht1b_human Human No 9.2 EC50 = 0.6 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
434 13 4 4 4.7 NCCc1c[nH]c2ccc(OCCCCCCOc3ccc4[nH]cc(CCN)c4c3)cc12
CHEMBL148022 5ht1b_human Human No 9.1 EC50 = 0.9 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3cccc(COc4ccc5[nH]cc(CCN)c5c4)c3)cc12
CHEMBL147677 5ht1b_human Human No 8.8 EC50 = 1.6 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
464 12 6 5 2.4 NCCc1c[nH]c2ccc(OCCNC(=O)NCCOc3ccc4[nH]cc(CCN)c4c3)cc12
CHEMBL1183904 5ht1b_human Human No 8.7 EC50 = 1.9 nM Bind
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3ccc(C)cc3C)CC2)cc1N1CCN(C)CC1
CHEMBL323986 5ht1b_human Human No 8.7 EC50 = 1.9 nM Bind
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3ccc(C)cc3C)CC2)cc1N1CCN(C)CC1
CHEMBL111302 5ht1b_human Human No 8.0 EC50 = 10 nM Bind
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3c(C)cccc3C)CC2)cc1N1CCN(C)CC1
CHEMBL1180017 5ht1b_human Human No 8.0 EC50 = 10 nM Bind
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3c(C)cccc3C)CC2)cc1N1CCN(C)CC1
CHEMBL63258 5ht1b_human Human No 5.0 EC50 = 10000 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
451 8 1 5 4.6 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1
CHEMBL294547 5ht1b_human Human No 6.9 EC50 = 120 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL2104993 5ht1b_human Human Yes 6.9 EC50 = 120 nM Funct
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1
CHEMBL304857 5ht1b_human Human No 5.9 EC50 = 1400 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL1185 5ht1b_human Human Yes 7.8 EC50 = 15.7 nM Funct
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C
CHEMBL470849 5ht1b_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
416 5 1 5 3.6 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5)CC3)cccc2n1
CHEMBL65321 5ht1b_human Human No 5.8 EC50 = 1500 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1cccc(F)c1
CHEMBL64004 5ht1b_human Human No 5.8 EC50 = 1700 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1
CHEMBL4207355 5ht1b_human Human No 6.8 EC50 = 180 nM Funct
Partial agonist activity at 5-HT1B receptor (unknown origin) by Tango assayPartial agonist activity at 5-HT1B receptor (unknown origin) by Tango assay
307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1
CHEMBL1290596 5ht1b_human Human No 6.7 EC50 = 199.5 nM Funct
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
414 4 1 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4CCC(=O)N5)CC3)cccc2n1
CHEMBL148314 5ht1b_human Human No 8.7 EC50 = 2.1 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccccc3COc3ccc4[nH]cc(CCN)c4c3)cc12
CHEMBL120055 5ht1b_human Human No 8.7 EC50 = 2.1 nM Funct
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonistThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonist
392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1
CHEMBL321818 5ht1b_human Human No 8.7 EC50 = 2.1 nM Funct
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonistThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonist
392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1
CHEMBL128699 5ht1b_human Human No 7.6 EC50 = 25 nM Funct
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
486 5 0 5 4.2 Cc1cc(C)c(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c(C)c1
CHEMBL129813 5ht1b_human Human No 7.6 EC50 = 25 nM Funct
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
502 5 0 7 3.1 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6c5OCCO6)CC4)cc23)CC1
CHEMBL469376 5ht1b_human Human No 7.6 EC50 = 25.1 nM Funct
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
444 5 0 5 4.0 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1
CHEMBL39 5ht1b_rat Rat Yes 7.6 EC50 = 26 nM Bind
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL56 5ht1b_human Human Yes 6.6 EC50 = 260 nM Funct
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL2112660 5ht1b_human Human No 7.6 EC50 = 28 nM Funct
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
469 5 0 6 3.2 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5ccccc5C#N)CC4)cc23)CC1
CHEMBL4212246 5ht1b_human Human No 7.5 EC50 = 29 nM Funct
Partial agonist activity at 5-HT1B receptor (unknown origin) by Tango assayPartial agonist activity at 5-HT1B receptor (unknown origin) by Tango assay
279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1
CHEMBL63167 5ht1b_human Human No 6.5 EC50 = 290 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
485 7 1 4 5.7 FC1(Cc2ccccc2C(F)(F)F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL144030 5ht1b_human Human No 8.5 EC50 = 3 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12
CHEMBL338015 5ht1b_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
504 7 0 7 3.3 COc1cccc(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c1OC
CHEMBL39 5ht1b_human Human Yes 7.5 EC50 = 30 nM Bind
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampusInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1289164 5ht1b_human Human No 6.5 EC50 = 316.2 nM Funct
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
446 4 0 5 4.4 Cc1ccc2c(N3CCN(CCc4c(Cl)ccc5c4ccc(=O)n5C)CC3)cccc2n1
CHEMBL128 5ht1b_human Human Yes 7.4 EC50 = 38.3 nM Funct
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL1290597 5ht1b_human Human No 6.4 EC50 = 398.1 nM Funct
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
428 4 0 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4CCC(=O)N5C)CC3)cccc2n1
CHEMBL343196 5ht1b_human Human No 8.4 EC50 = 4 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
378 9 4 4 3.1 NCCc1c[nH]c2ccc(OCCOc3ccc4[nH]cc(CCN)c4c3)cc12
CHEMBL39 5ht1b_human Human Yes 8.3 EC50 = 4.7 nM Funct
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full AgonistThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht1b_human Human Yes 8.3 EC50 = 4.8 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL292779 5ht1b_human Human Yes 6.4 EC50 = 430 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1
CHEMBL63799 5ht1b_human Human No 6.4 EC50 = 440 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
449 8 1 4 5.3 Fc1cccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL432332 5ht1b_human Human No 6.4 EC50 = 450 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
417 7 1 4 4.6 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1
CHEMBL29951 5ht1b_human Human No 7.3 EC50 = 50 nM Funct
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
576 19 0 4 8.7 CCCN(CCC)C1CCc2cccc(OCCCCCCOc3cccc4c3CC(N(CCC)CCC)CC4)c2C1
CHEMBL1289047 5ht1b_human Human No 6.3 EC50 = 501.2 nM Funct
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
412 4 1 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5[nH]c(=O)ccc45)CC3)cccc2n1
CHEMBL67684 5ht1b_human Human No 6.3 EC50 = 510 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
445 8 1 4 5.7 CC(CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL433108 5ht1b_human Human No 5.3 EC50 = 5100 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
464 8 1 5 4.3 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL304008 5ht1b_rat Rat Yes 7.3 EC50 = 56 nM Funct
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1
CHEMBL4064865 5ht1b_human Human No 6.2 EC50 = 570 nM Bind
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
586 3 2 9 4.5 O=C1CCc2cc3cc(c2N1Cc1ccccc1)OC/C=C/CO[C@H]1C[C@@H](CO)N(C1)c1cc(n2ncc(Cl)c2n1)N3
CHEMBL472289 5ht1b_human Human No 8.2 EC50 = 6.3 nM Funct
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5C)CC3)cccc2n1
CHEMBL1289048 5ht1b_human Human No 7.2 EC50 = 63.1 nM Funct
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
426 4 0 5 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4ccc(=O)n5C)CC3)cccc2n1
CHEMBL469375 5ht1b_human Human No 7.2 EC50 = 63.1 nM Funct
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
430 5 0 5 3.7 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1
CHEMBL294732 5ht1b_human Human No 7.2 EC50 = 66 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL128 5ht1b_human Human Yes 7.1 EC50 = 77 nM Funct
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL63432 5ht1b_human Human No 6.1 EC50 = 810 nM Funct
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL194837 5ht1b_human Human No 9.7 IC50 = 0.2 nM Bind
Inhibitory concentration against 5-hydroxytryptamine 1B receptorInhibitory concentration against 5-hydroxytryptamine 1B receptor
447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12
CHEMBL442 5ht1b_rat Rat Yes 9.7 IC50 = 0.2 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL159396 5ht1b_human Human No 9.3 IC50 = 0.5 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
388 6 1 7 2.3 c1cnc(N2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1
CHEMBL147503 5ht1b_rat Rat Yes 9.3 IC50 = 0.5 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
457 6 3 5 4.0 COc1ccc(NC(=O)c2ccc(-c3ccc(C(=N)N)cc3C)cc2)cc1N1CCN(C)CC1
CHEMBL128 5ht1b_human Human Yes 9.3 IC50 = 0.5 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL26379 5ht1b_rat Rat Yes 9.1 IC50 = 0.8 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1
CHEMBL1732 5ht1b_rat Rat Yes 9.1 IC50 = 0.8 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL146735 5ht1b_rat Rat Yes 9.0 IC50 = 0.9 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
497 6 1 7 5.0 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1
CHEMBL26378 5ht1b_rat Rat Yes 8.9 IC50 = 1.2 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
214 1 3 2 2.3 Oc1ccc2[nH]cc(C3=CCNCC3)c2c1
CHEMBL296161 5ht1b_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12
CHEMBL296161 5ht1b_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12
CHEMBL147071 5ht1b_rat Rat Yes 8.9 IC50 = 1.3 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
458 6 2 5 3.8 COc1ccc(NC(=O)c2ccc(-c3ccc(C(N)=O)cc3C)cc2)cc1N1CCN(C)CC1
CHEMBL296161 5ht1b_human Human No 8.9 IC50 = 1.4 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12
CHEMBL15928 5ht1b_rat Rat Yes 8.8 IC50 = 1.6 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C
CHEMBL15928 5ht1b_rat Rat Yes 8.8 IC50 = 1.6 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C
CHEMBL26906 5ht1b_rat Rat Yes 8.7 IC50 = 1.9 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
216 1 2 1 2.7 Fc1ccc2[nH]cc(C3=CCNCC3)c2c1
CHEMBL128 5ht1b_human Human Yes 8.0 IC50 = 10 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL157138 5ht1b_rat Rat Yes 8.0 IC50 = 10 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC
CHEMBL357634 5ht1b_human Human No 8.0 IC50 = 10 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
478 8 1 6 3.5 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)S(=O)(=O)c1ccccc1
CHEMBL151420 5ht1b_rat Rat No 8.0 IC50 = 10 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
529 8 1 7 5.4 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc(OCCF)c(N5CCN(C)CC5)c4)cc3)c(C)c2)no1
CHEMBL147853 5ht1b_human Human No 7.0 IC50 = 100 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
458 10 3 6 3.3 OC[C@@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL3126382 5ht1b_human Human No 7.0 IC50 = 100 nM Bind
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1
CHEMBL3139683 5ht1b_human Human No 7.0 IC50 = 100 nM Bind
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1
CHEMBL149488 5ht1b_human Human No 7.0 IC50 = 100 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
485 9 2 6 4.2 CC(=O)Nc1ccc(CN(C)C2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL434125 5ht1b_human Human No 7.0 IC50 = 100 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
443 9 3 5 4.1 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4ccnc4)cc23)CC1)c1ccccc1
CHEMBL116031 5ht1b_human Human No 7.0 IC50 = 100 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
432 8 1 5 3.7 Fc1ccccc1CCN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL61818 5ht1b_rat Rat No 6.0 IC50 = 1000 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
449 6 0 5 4.8 Cn1c(=O)sc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21
CHEMBL3608450 5ht1b_human Human No 6.0 IC50 = 1000 nM Bind
Agonist activity at 5HT1B receptor (unknown origin)Agonist activity at 5HT1B receptor (unknown origin)
415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4
CHEMBL267930 5ht1b_rat Rat Yes 6.0 IC50 = 1000 nM Bind
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1
CHEMBL1195096 5ht1b_rat Rat No 6.0 IC50 = 1000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1
CHEMBL553833 5ht1b_rat Rat No 6.0 IC50 = 1000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1
CHEMBL28312 5ht1b_rat Rat No 6.0 IC50 = 1000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1
CHEMBL48925 5ht1b_rat Rat No 6.0 IC50 = 1000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1
CHEMBL283606 5ht1b_rat Rat Yes 6.0 IC50 = 1000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1
CHEMBL51561 5ht1b_rat Rat No 6.0 IC50 = 1000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1
CHEMBL56990 5ht1b_rat Rat No 6.0 IC50 = 1000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1
CHEMBL63258 5ht1b_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
451 8 1 5 4.6 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1
CHEMBL63432 5ht1b_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL65215 5ht1b_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
482 8 1 5 4.5 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1
CHEMBL11592 5ht1b_rat Rat Yes 5.0 IC50 = 10000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL301060 5ht1b_rat Rat Yes 5.0 IC50 = 10000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL1178932 5ht1b_rat Rat No 5.0 IC50 = 10000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL50530 5ht1b_rat Rat No 5.0 IC50 = 10000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL26975 5ht1b_rat Rat No 5.0 IC50 = 10000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL52485 5ht1b_rat Rat No 5.0 IC50 = 10000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL11592 5ht1b_rat Rat Yes 5.0 IC50 = 10000 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL301060 5ht1b_rat Rat Yes 5.0 IC50 = 10000 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL300692 5ht1b_rat Rat No 5.0 IC50 = 10000 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
374 3 0 4 4.3 Cc1ccc2c(c1)nc(N1CCN(Cc3ccc(F)cc3)CC1)c1cccn12
CHEMBL1911194 5ht1b_human Human No 5.0 IC50 = 10000 nM Bind
Inhibition of 5-HT1BInhibition of 5-HT1B
374 2 2 4 3.8 Cc1nnc(-c2ccc(C)c(-c3ccc4c(c3)NC(=O)C43CCOCC3)c2)[nH]1
CHEMBL285010 5ht1b_rat Rat No 4.0 IC50 = 100000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
233 2 0 3 2.1 COc1cccc2c1CC(N1CCCC1)CO2
CHEMBL164035 5ht1b_human Human No 7.0 IC50 = 102 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
471 8 1 6 3.1 CN(C)C(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL54720 5ht1b_rat Rat No 6.0 IC50 = 1023.3 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
348 3 0 5 3.9 c1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1
CHEMBL54720 5ht1b_rat Rat No 6.0 IC50 = 1023.3 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
348 3 0 5 3.9 c1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1
CHEMBL65736 5ht1b_rat Rat No 5.0 IC50 = 10232.9 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
312 3 0 5 3.1 c1cc2c(N3CCN(CC4CC4)CC3)nc3ccsc3n2c1
CHEMBL493 5ht1b_rat Rat Yes 7.0 IC50 = 103 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C
CHEMBL331304 5ht1b_rat Rat No 7.0 IC50 = 106 nM Bind
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
270 1 1 4 2.0 Fc1cccc2nc(N3CCNCC3)c3cccn3c12
CHEMBL64948 5ht1b_rat Rat No 6.0 IC50 = 1096.5 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
300 3 0 5 3.1 CCCN1CCN(c2nc3ccsc3n3cccc23)CC1
CHEMBL65367 5ht1b_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cellsDisplacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cells
400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL128 5ht1b_human Human Yes 8.0 IC50 = 11 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL65367 5ht1b_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL128 5ht1b_human Human Yes 8.0 IC50 = 11 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL423599 5ht1b_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
442 8 1 5 3.7 CC(=O)N(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1
CHEMBL65367 5ht1b_human Human No 8.0 IC50 = 11 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL65367 5ht1b_human Human No 8.0 IC50 = 11 nM Funct
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL128 5ht1b_rat Rat Yes 7.0 IC50 = 110 nM Bind
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL118012 5ht1b_human Human No 7.0 IC50 = 110 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL161066 5ht1b_human Human No 7.0 IC50 = 110 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
401 8 2 6 2.8 c1cc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)ccn1
CHEMBL147907 5ht1b_human Human No 7.0 IC50 = 110 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
427 8 2 4 5.1 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4ccnc4)cc23)CC1)c1ccccc1
CHEMBL364005 5ht1b_human Human Yes 7.0 IC50 = 110 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor in calfInhibitory activity against 5-hydroxytryptamine 1B receptor in calf
246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C
CHEMBL3645480 5ht1b_rat Rat No 6.0 IC50 = 1100 nM Bind
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
308 3 2 3 3.2 CN1CCC(c2c[nH]c3ccc(/N=C(\N)c4ccco4)cc23)C1
CHEMBL422453 5ht1b_rat Rat No 5.0 IC50 = 11000 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
261 3 0 3 2.9 CCCN1CCCC12COc1cccc(OC)c1C2
CHEMBL2110300 5ht1b_human Human No 7.0 IC50 = 112.2 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
313 4 2 3 2.6 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1
CHEMBL334498 5ht1b_rat Rat No 5.0 IC50 = 11200 nM Bind
Compound was evaluated for binding affinity on 5-HT1B receptors using rat cortex+striatum+ globus pallidus,[ 3H]-5-OH-tryptamine, and serotonin for NSB.Compound was evaluated for binding affinity on 5-HT1B receptors using rat cortex+striatum+ globus pallidus,[ 3H]-5-OH-tryptamine, and serotonin for NSB.
426 7 1 4 4.2 COc1cccc2c1CC1(CCCCN1CCCCNC(=O)c1ccc(F)cc1)CO2
CHEMBL2368255 5ht1b_human Human No 6.0 IC50 = 1122.0 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
340 4 3 3 2.2 CC1(C)NC(=O)N(CCc2ccc3[nH]cc([C@H]4C[C@H](N)C4)c3c2)C1=O
CHEMBL65974 5ht1b_rat Rat No 5.0 IC50 = 11220.2 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
272 1 0 5 2.3 CN1CCN(c2nc3ccsc3n3cccc23)CC1
CHEMBL274922 5ht1b_rat Rat No 7.0 IC50 = 113 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
490 5 3 5 3.4 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(C(N)=O)cc34)CC2)cc1N1CCN(C)CC1
CHEMBL118012 5ht1b_human Human No 6.9 IC50 = 114 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL39 5ht1b_human Human Yes 7.9 IC50 = 12 nM Bind
Binding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assayBinding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL2376490 5ht1b_rat Rat No 7.9 IC50 = 12 nM Bind
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
294 2 2 2 4.6 Cc1[nH]c2ccc(-c3ccsc3)cc2c1C1=CCNCC1
CHEMBL349185 5ht1b_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
390 8 2 6 3.0 c1cc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)co1
CHEMBL342805 5ht1b_human Human No 6.9 IC50 = 120 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
487 10 3 7 3.6 NC(=O)OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL280000 5ht1b_rat Rat No 6.9 IC50 = 120 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
475 6 2 4 4.8 COc1ccc(NC(=O)N2CCC(CCc3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1
CHEMBL115750 5ht1b_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
432 8 1 5 3.7 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL117046 5ht1b_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
414 8 2 5 3.9 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL115750 5ht1b_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
432 8 1 5 3.7 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL344537 5ht1b_human Human No 5.9 IC50 = 1200 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
490 11 2 6 4.3 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(Cn4cncn4)cc23)CC1)c1ccc(F)cc1
CHEMBL416688 5ht1b_human Human No 5.9 IC50 = 1200 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
446 8 1 5 4.2 CN(Cc1ccccc1)C1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL63432 5ht1b_human Human No 5.9 IC50 = 1200 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL2368262 5ht1b_human Human No 5.9 IC50 = 1202.3 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
368 5 2 3 2.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CCN4C(=O)NC(C)(C)C4=O)cc32)C1
CHEMBL117046 5ht1b_human Human No 6.9 IC50 = 125 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
414 8 2 5 3.9 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL348815 5ht1b_human Human No 6.9 IC50 = 125 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
414 9 2 5 3.4 c1ccc(CCNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL49 5ht1b_rat Rat Yes 4.9 IC50 = 12589.3 nM Bind
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL53416 5ht1b_rat Rat No 4.9 IC50 = 12882.5 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
342 3 0 4 3.8 c1ccc(CN2CCN(c3nc4ccccc4n4cccc34)CC2)cc1
CHEMBL723 5ht1b_rat Rat Yes 5.9 IC50 = 1295 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O
CHEMBL162463 5ht1b_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
386 6 1 5 3.5 c1ccc(N2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL163462 5ht1b_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
443 8 2 6 2.5 NC(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL351346 5ht1b_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
414 7 1 5 4.1 CC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL147818 5ht1b_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
471 10 2 6 4.0 CN(C)C[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL2114040 5ht1b_human Human No 7.9 IC50 = 13 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
446 8 1 5 4.2 CN(Cc1ccccc1)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@@H]1F
CHEMBL301765 5ht1b_rat Rat No 7.9 IC50 = 13.8 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
258 1 1 5 2.0 c1cc2c(N3CCNCC3)nc3ccsc3n2c1
CHEMBL301765 5ht1b_rat Rat No 7.9 IC50 = 13.8 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
258 1 1 5 2.0 c1cc2c(N3CCNCC3)nc3ccsc3n2c1
CHEMBL347665 5ht1b_human Human No 6.9 IC50 = 130 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
425 7 1 6 3.4 N#Cc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL11265 5ht1b_rat Rat No 5.9 IC50 = 1300 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL341854 5ht1b_human Human No 5.9 IC50 = 1300 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
458 10 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(Cn4cncn4)cc23)CC1)c1ccccc1
CHEMBL64003 5ht1b_human Human No 5.9 IC50 = 1300 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
435 7 1 4 4.9 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1
CHEMBL53573 5ht1b_rat Rat No 4.9 IC50 = 13182.6 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
343 3 0 5 3.2 c1ccc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)cc1
CHEMBL349824 5ht1b_rat Rat No 5.9 IC50 = 1320 nM Bind
Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol, binds to 5-hydroxytryptamine 1B receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol, binds to 5-hydroxytryptamine 1B receptor at 1 uM
259 3 0 3 3.0 CCCN1CCC=C2c3c(OC)cccc3OCC21
CHEMBL279320 5ht1b_rat Rat No 6.9 IC50 = 133 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
497 10 3 5 4.3 COc1ccc(NC(=O)NCCN2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1OCCN(C)C
CHEMBL348811 5ht1b_human Human No 5.9 IC50 = 1349.0 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
271 4 2 2 2.0 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC(N)=O)cc32)C1
CHEMBL157101 5ht1b_rat Rat Yes 4.9 IC50 = 13539 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1
CHEMBL621 5ht1b_rat Rat Yes 5.9 IC50 = 1356 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2
CHEMBL296419 5ht1b_rat Rat Yes 5.9 IC50 = 1387 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2
CHEMBL4128926 5ht1b_rat Rat No 7.9 IC50 = 14 nM Bind
Displacement of [125I]-CYP from rat brain 5-HT1B receptor after 120 mins by scintillation counting analysisDisplacement of [125I]-CYP from rat brain 5-HT1B receptor after 120 mins by scintillation counting analysis
583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12
CHEMBL343648 5ht1b_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
442 9 2 5 4.7 C[C@@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL63167 5ht1b_human Human No 7.9 IC50 = 14 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
485 7 1 4 5.7 FC1(Cc2ccccc2C(F)(F)F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL159332 5ht1b_human Human Yes 7.8 IC50 = 14.5 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C
CHEMBL146131 5ht1b_human Human No 6.9 IC50 = 140 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
458 10 3 6 3.3 OC[C@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL2376491 5ht1b_rat Rat No 6.9 IC50 = 140 nM Bind
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1
CHEMBL146729 5ht1b_human Human No 6.9 IC50 = 140 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
415 8 2 6 3.3 c1cc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)ccn1
CHEMBL146891 5ht1b_human Human No 6.9 IC50 = 140 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
415 8 2 6 3.3 c1cncc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL147555 5ht1b_human Human No 6.9 IC50 = 140 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
506 9 1 7 3.7 CN(Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL148325 5ht1b_human Human No 6.9 IC50 = 140 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
457 7 2 5 4.3 CN(C(=O)Nc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL304857 5ht1b_human Human No 6.9 IC50 = 140 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL423212 5ht1b_human Human No 6.9 IC50 = 140 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
434 8 1 6 4.3 CN(Cc1cccs1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL304857 5ht1b_human Human No 6.9 IC50 = 140 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL154787 5ht1b_rat Rat No 5.9 IC50 = 1400 nM Bind
In vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membrane
458 7 1 8 4.2 COc1ccccc1C1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1
CHEMBL3084967 5ht1b_human Human No 6.9 IC50 = 141.3 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
327 5 2 3 2.7 CN(C)[C@H]1C[C@H](Cc2c[nH]c3ccc(C[C@H]4COC(=O)N4)cc23)C1
CHEMBL418678 5ht1b_rat Rat No 4.8 IC50 = 14454.4 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
366 3 0 5 4.0 Fc1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1
CHEMBL416662 5ht1b_rat Rat No 4.8 IC50 = 14454.4 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
420 3 0 6 4.2 Clc1ccc2c(c1)nc(N1CCN(Cc3ccc4c(c3)OCO4)CC1)c1cccn12
CHEMBL304857 5ht1b_human Human No 6.8 IC50 = 145 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL274001 5ht1b_human Human No 6.8 IC50 = 145 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
310 5 2 5 1.6 c1cc2[nH]cc(CCCN3CCNCC3)c2cc1-n1cnnc1
CHEMBL420874 5ht1b_human Human No 6.8 IC50 = 145 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL420874 5ht1b_human Human No 6.8 IC50 = 146 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL62366 5ht1b_rat Rat No 4.8 IC50 = 14791.1 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
348 2 0 5 4.0 CN1CCN(c2nc3cc(-c4ccccc4)sc3n3cccc23)CC1
CHEMBL331612 5ht1b_human Human No 7.8 IC50 = 15 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
309 5 1 4 3.2 c1cc2[nH]cc(CCCN3CCCCC3)c2cc1-n1cnnc1
CHEMBL1201356 5ht1b_rat Rat Yes 7.8 IC50 = 15 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO
CHEMBL294732 5ht1b_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cellsDisplacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cells
417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL331612 5ht1b_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
309 5 1 4 3.2 c1cc2[nH]cc(CCCN3CCCCC3)c2cc1-n1cnnc1
CHEMBL159683 5ht1b_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
414 8 1 5 3.9 CN(Cc1ccccc1)C[C@@H]1CCCN1CCc1c[nH]c2ccc(-n3cnnc3)cc12
CHEMBL294732 5ht1b_human Human No 7.8 IC50 = 15 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL294732 5ht1b_human Human No 7.8 IC50 = 15 nM Funct
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL304008 5ht1b_rat Rat Yes 7.8 IC50 = 15 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1
CHEMBL146628 5ht1b_human Human No 6.8 IC50 = 150 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
458 10 3 6 3.9 OCCC(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL313714 5ht1b_human Human Yes 6.8 IC50 = 150 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1
CHEMBL356315 5ht1b_human Human No 6.8 IC50 = 150 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
458 9 3 6 3.9 C[C@H](O)[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL27403 5ht1b_rat Rat Yes 6.8 IC50 = 150 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F
CHEMBL53490 5ht1b_rat Rat No 6.8 IC50 = 151.4 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
253 1 1 5 1.3 c1cnc2c(c1)nc(N1CCNCC1)c1cccn12
CHEMBL161694 5ht1b_human Human No 5.8 IC50 = 1513.6 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
310 4 1 4 3.3 Cc1noc(Cc2ccc3[nH]cc([C@H]4C[C@H](N(C)C)C4)c3c2)n1
CHEMBL11409 5ht1b_human Human No 5.8 IC50 = 1584.9 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
497 8 0 6 3.9 CCCN1CCN(CCCCN2C(=O)CC3(CCCC3)CC2=O)CC12COc1cccc(OC)c1C2
CHEMBL128 5ht1b_human Human Yes 7.8 IC50 = 16 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL128 5ht1b_human Human Yes 7.8 IC50 = 16 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL67460 5ht1b_human Human No 7.8 IC50 = 16 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
449 8 1 4 5.3 Fc1ccccc1CCC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL39 5ht1b_human Human Yes 7.8 IC50 = 16 nM Bind
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1963527 5ht1b_rat Rat Yes 6.8 IC50 = 160 nM Bind
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
336 3 2 3 4.0 CN1CC=C(c2c[nH]c3ccc(/N=C(\N)c4cccs4)cc23)CC1
CHEMBL146132 5ht1b_human Human No 6.8 IC50 = 160 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
444 9 3 6 3.5 OC[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL305301 5ht1b_human Human No 5.8 IC50 = 1600 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
468 8 1 5 3.9 Fc1cccc(CCN2CCN(CC(F)(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL2110300 5ht1b_human Human No 6.8 IC50 = 162.2 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
313 4 2 3 2.6 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1
CHEMBL349390 5ht1b_human Human No 6.8 IC50 = 165 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
457 9 3 6 3.4 CC(=O)Nc1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL351303 5ht1b_human Human No 6.8 IC50 = 165 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
430 9 3 6 2.9 OC[C@@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1
CHEMBL117633 5ht1b_human Human No 6.8 IC50 = 166 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
414 8 1 5 3.5 c1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL120216 5ht1b_rat Rat Yes 6.8 IC50 = 167 nM Bind
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
270 1 1 4 2.0 Fc1ccc2c(c1)nc(N1CCNCC1)c1cccn12
CHEMBL348962 5ht1b_human Human No 7.8 IC50 = 17 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
443 9 2 6 3.3 CNCC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL146502 5ht1b_human Human No 6.8 IC50 = 170 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
442 9 2 5 4.4 C[C@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL146023 5ht1b_human Human No 6.8 IC50 = 170 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
485 10 3 6 3.9 CC(=O)Nc1ccc(CCNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL117633 5ht1b_human Human No 6.8 IC50 = 170 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
414 8 1 5 3.5 c1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL333089 5ht1b_human Human No 6.8 IC50 = 170 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
471 9 2 6 3.5 CC(=O)Nc1cccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL2114038 5ht1b_human Human No 6.8 IC50 = 170 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
500 8 2 5 4.9 F[C@H]1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC[C@@H]1NCc1ccccc1C(F)(F)F
CHEMBL1065 5ht1b_rat Rat Yes 6.8 IC50 = 177 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO
CHEMBL128 5ht1b_rat Rat Yes 7.8 IC50 = 18 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL162805 5ht1b_human Human No 7.8 IC50 = 18 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
390 7 1 6 3.1 c1coc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL163573 5ht1b_human Human No 7.8 IC50 = 18 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
401 7 1 6 2.9 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1
CHEMBL352159 5ht1b_human Human No 7.8 IC50 = 18 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
430 7 1 5 3.8 S=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1Cc1ccccc1
CHEMBL145982 5ht1b_human Human No 7.8 IC50 = 18 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
492 9 1 6 3.7 CN(CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)S(=O)(=O)c1ccccc1
CHEMBL2110299 5ht1b_human Human No 7.7 IC50 = 18.2 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
285 3 3 3 2.0 N[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1
CHEMBL304438 5ht1b_rat Rat No 6.8 IC50 = 180 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
381 5 0 5 2.4 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCC(=O)N3C)CC1
CHEMBL364005 5ht1b_rat Rat Yes 6.8 IC50 = 180 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor in ratInhibitory activity against 5-hydroxytryptamine 1B receptor in rat
246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C
CHEMBL433108 5ht1b_human Human No 5.8 IC50 = 1800 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
464 8 1 5 4.3 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL428892 5ht1b_rat Rat Yes 6.7 IC50 = 182.0 nM Bind
Binding affinity towards 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity towards 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
356 2 0 4 4.4 CSc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2
CHEMBL313714 5ht1b_human Human Yes 6.7 IC50 = 185 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1
CHEMBL81 5ht1b_rat Rat Yes 5.7 IC50 = 1861 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O
CHEMBL63713 5ht1b_rat Rat No 4.7 IC50 = 18620.9 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
430 4 0 5 4.9 FC(F)(F)c1ccccc1CCN1CCN(c2nc3ccsc3n3cccc23)CC1
CHEMBL116161 5ht1b_human Human No 7.7 IC50 = 19 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
450 7 2 6 3.6 CC1(C)CCCN(CC2(O)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)C1
CHEMBL19215 5ht1b_rat Rat Yes 7.7 IC50 = 19 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C
CHEMBL294547 5ht1b_human Human No 7.7 IC50 = 19 nM Bind
Displacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cellsDisplacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cells
399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL294547 5ht1b_human Human No 7.7 IC50 = 19 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL294547 5ht1b_human Human No 7.7 IC50 = 19 nM Funct
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL4207355 5ht1b_human Human No 5.7 IC50 = 1900 nM Funct
Antagonist activity at 5-HT1B receptor (unknown origin) by Tango assayAntagonist activity at 5-HT1B receptor (unknown origin) by Tango assay
307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1
CHEMBL62902 5ht1b_rat Rat No 4.7 IC50 = 19054.6 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
478 3 0 5 6.6 FC(F)(F)c1cccc(N2CCN(c3nc4scc(-c5ccccc5)c4n4cccc34)CC2)c1
CHEMBL299634 5ht1b_rat Rat No 4.7 IC50 = 19054.6 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
376 3 0 4 4.5 Clc1ccc2c(c1)nc(N1CCN(Cc3ccccc3)CC1)c1cccn12
CHEMBL726 5ht1b_rat Rat Yes 5.7 IC50 = 1912 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F
CHEMBL64903 5ht1b_rat Rat No 4.7 IC50 = 19498.5 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
380 4 0 5 4.0 Fc1ccc(CN2CCN(Cc3nc4ccsc4n4cccc34)CC2)cc1
CHEMBL299097 5ht1b_rat Rat No 4.7 IC50 = 19498.5 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
343 3 0 5 3.3 C=CCN1CCN(c2nc3ccc4ncccc4c3n3cccc23)CC1
CHEMBL762 5ht1b_rat Rat Yes 8.7 IC50 = 2 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL281350 5ht1b_rat Rat Yes 8.7 IC50 = 2 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C
CHEMBL18785 5ht1b_rat Rat Yes 8.7 IC50 = 2 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1
CHEMBL15933 5ht1b_rat Rat No 8.7 IC50 = 2.1 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
494 4 1 6 5.6 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)C4(CCN(C)CC4)CO5)cc3)c(C)c2)no1
CHEMBL161176 5ht1b_human Human No 8.6 IC50 = 2.4 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
457 8 2 6 3.5 CC(=O)Nc1cccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL348304 5ht1b_human Human No 8.6 IC50 = 2.7 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
401 8 1 5 4.0 c1ccc(COC[C@@H]2CCCN2CCc2c[nH]c3ccc(-n4cnnc4)cc23)cc1
CHEMBL119443 5ht1b_rat Rat Yes 8.6 IC50 = 2.8 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C
CHEMBL1909065 5ht1b_rat Rat Yes 8.5 IC50 = 3.0 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC
CHEMBL60885 5ht1b_rat Rat No 7.7 IC50 = 20 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
369 5 1 6 3.4 COc1ccccc1N1CCN(CCc2ccc3nc(O)sc3c2)CC1
CHEMBL161723 5ht1b_human Human No 7.7 IC50 = 20 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
418 7 1 5 3.6 Fc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL349041 5ht1b_human Human No 7.7 IC50 = 20 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
390 8 2 6 3.0 c1coc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)c1
CHEMBL64167 5ht1b_rat Rat No 6.7 IC50 = 200 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
353 4 0 5 3.0 Cn1c(=O)sc2cc(CCN3CCN(c4ccccc4)CC3)ccc21
CHEMBL64878 5ht1b_rat Rat No 6.7 IC50 = 200 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
397 7 1 6 4.2 COc1ccccc1N1CCN(CCCCc2ccc3nc(O)sc3c2)CC1
CHEMBL423022 5ht1b_human Human No 6.7 IC50 = 200 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
458 9 3 6 3.9 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@H](O)c1ccccc1
CHEMBL2376483 5ht1b_rat Rat No 6.7 IC50 = 200 nM Bind
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1
CHEMBL148085 5ht1b_human Human No 6.7 IC50 = 200 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
418 8 1 6 3.9 CN(Cc1ccoc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL280586 5ht1b_rat Rat No 5.7 IC50 = 2000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL54266 5ht1b_rat Rat No 5.7 IC50 = 2000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL1178932 5ht1b_rat Rat No 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL50530 5ht1b_rat Rat No 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL1178987 5ht1b_rat Rat No 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL52785 5ht1b_rat Rat No 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL1185501 5ht1b_rat Rat No 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL417550 5ht1b_rat Rat No 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL26018 5ht1b_rat Rat No 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL300735 5ht1b_rat Rat No 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL27650 5ht1b_rat Rat No 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL50188 5ht1b_rat Rat No 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL283606 5ht1b_rat Rat Yes 4.7 IC50 = 20000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1
CHEMBL283606 5ht1b_rat Rat Yes 4.7 IC50 = 20000 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1
CHEMBL2368257 5ht1b_human Human No 6.7 IC50 = 204.2 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
327 4 1 3 3.0 CN1C(=O)OCC1Cc1ccc2[nH]cc([C@H]3C[C@H](N(C)C)C3)c2c1
CHEMBL2368261 5ht1b_human Human No 6.7 IC50 = 204.2 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
387 5 1 3 3.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CCN4C(=O)c5ccccc5C4=O)cc32)C1
CHEMBL299231 5ht1b_rat Rat No 6.7 IC50 = 204.2 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
293 3 0 5 2.2 C=CCN1CCN(c2nc3cccnc3n3cccc23)CC1
CHEMBL1559 5ht1b_rat Rat Yes 4.7 IC50 = 20600 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1
CHEMBL91 5ht1b_rat Rat Yes 4.7 IC50 = 20600 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1
CHEMBL324287 5ht1b_human Human No 6.7 IC50 = 209 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
400 7 1 5 3.5 CN(Cc1ccccc1)[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1
CHEMBL28178 5ht1b_rat Rat No 7.7 IC50 = 21 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
320 1 1 4 2.9 FC(F)(F)c1ccc2c(c1)nc(N1CCNCC1)c1cccn12
CHEMBL143890 5ht1b_human Human No 6.7 IC50 = 210 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
458 9 3 6 3.9 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](O)c1ccccc1
CHEMBL145815 5ht1b_human Human No 6.7 IC50 = 210 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
458 10 2 6 4.1 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL423749 5ht1b_human Human No 6.7 IC50 = 210 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
458 9 2 6 3.8 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](CO)c1ccccc1
CHEMBL324287 5ht1b_human Human No 6.7 IC50 = 210 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
400 7 1 5 3.5 CN(Cc1ccccc1)[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1
CHEMBL2112862 5ht1b_human Human No 6.7 IC50 = 210 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
456 7 3 6 3.4 O[C@@H]1Cc2ccccc2[C@H]1NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL4212246 5ht1b_human Human No 5.7 IC50 = 2100 nM Funct
Antagonist activity at 5-HT1B receptor (unknown origin) by Tango assayAntagonist activity at 5-HT1B receptor (unknown origin) by Tango assay
279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1
CHEMBL67367 5ht1b_human Human No 5.7 IC50 = 2100 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
464 8 1 5 4.5 CN(Cc1ccccc1)C1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL42 5ht1b_rat Rat Yes 5.7 IC50 = 2109 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL422366 5ht1b_human Human No 7.7 IC50 = 22 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
401 7 1 6 2.9 c1cncc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL63799 5ht1b_human Human No 7.7 IC50 = 22 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
449 8 1 4 5.3 Fc1cccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL2114039 5ht1b_human Human No 6.7 IC50 = 220 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
514 8 1 5 5.2 CN(Cc1ccccc1C(F)(F)F)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@@H]1F
CHEMBL2115112 5ht1b_human Human No 6.7 IC50 = 220 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
514 8 1 5 5.2 CN(Cc1ccccc1C(F)(F)F)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@H]1F
CHEMBL91534 5ht1b_human Human No 6.7 IC50 = 220 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
446 8 1 5 4.2 CN(Cc1ccccc1)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@H]1F
CHEMBL2203713 5ht1b_human Human No 5.7 IC50 = 2200 nM Bind
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1
CHEMBL1201049 5ht1b_rat Rat Yes 4.7 IC50 = 22034 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL808 5ht1b_rat Rat Yes 4.7 IC50 = 22034 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL422283 5ht1b_rat Rat No 5.7 IC50 = 2210 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
454 6 0 5 4.3 COc1cccc2c1CC1(CCCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL15965 5ht1b_rat Rat No 6.7 IC50 = 223 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
508 7 3 5 4.1 COc1ccc(NC(=O)NCCN2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1N1CCN(C)CC1
CHEMBL11262 5ht1b_human Human No 4.6 IC50 = 22908.7 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
277 7 0 3 3.4 CCCN(CCC)CC1COc2cccc(OC)c2C1
CHEMBL276928 5ht1b_rat Rat No 7.6 IC50 = 23 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
462 2 2 3 5.1 CN1CCC2(CC1)COc1ccc(NC(=O)N3CCC(c4c[nH]c5ccc(F)cc45)CC3)cc12
CHEMBL162858 5ht1b_human Human No 7.6 IC50 = 23 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
401 7 1 6 2.9 c1cc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)ccn1
CHEMBL146285 5ht1b_human Human No 6.6 IC50 = 230 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
446 8 2 5 4.6 CC(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1
CHEMBL305660 5ht1b_rat Rat Yes 5.6 IC50 = 2314 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1
CHEMBL327197 5ht1b_rat Rat No 6.6 IC50 = 232 nM Bind
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
266 1 0 4 2.2 CN1CCN(c2nc3ccccc3n3cccc23)CC1
CHEMBL279646 5ht1b_rat Rat No 6.6 IC50 = 233 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
451 4 2 4 4.1 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)C2)cc1N1CCN(C)CC1
CHEMBL302447 5ht1b_rat Rat No 4.6 IC50 = 23988.3 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
424 4 0 5 5.5 c1ccc(CN2CCN(c3nc4scc(-c5ccccc5)c4n4cccc34)CC2)cc1
CHEMBL1255837 5ht1b_rat Rat Yes 7.6 IC50 = 24 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O
CHEMBL601773 5ht1b_rat Rat Yes 7.6 IC50 = 24 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O
CHEMBL147660 5ht1b_human Human No 7.6 IC50 = 24 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
499 10 2 6 4.5 CC(=O)Nc1ccc(CN(C)CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL357007 5ht1b_human Human No 7.6 IC50 = 24 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
420 9 1 5 4.4 CC(C)=CCCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL3099899 5ht1b_rat Rat No 5.6 IC50 = 2400 nM Bind
Inhibition of rat 5-HT1B receptorInhibition of rat 5-HT1B receptor
493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC
CHEMBL54914 5ht1b_rat Rat No 6.6 IC50 = 245.5 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
267 1 0 5 1.6 CN1CCN(c2nc3cccnc3n3cccc23)CC1
CHEMBL356808 5ht1b_human Human No 7.6 IC50 = 25 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
454 8 2 5 4.7 c1ccc2c(c1)CCC2NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL293614 5ht1b_human Human No 7.6 IC50 = 25 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
449 8 1 4 5.3 Fc1ccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL42 5ht1b_rat Rat Yes 5.6 IC50 = 2500 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL119785 5ht1b_human Human No 6.6 IC50 = 251 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
471 9 2 6 3.5 CC(=O)Nc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL61869 5ht1b_rat Rat No 6.6 IC50 = 260 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
355 4 2 6 3.1 Oc1nc2ccc(CCN3CCN(c4ccccc4O)CC3)cc2s1
CHEMBL119785 5ht1b_human Human No 6.6 IC50 = 260 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
471 9 2 6 3.5 CC(=O)Nc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL161192 5ht1b_human Human No 6.6 IC50 = 260 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
414 9 2 5 3.5 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(Cn5cncn5)cc34)C2)cc1
CHEMBL147786 5ht1b_human Human No 6.6 IC50 = 260 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
392 8 1 5 3.5 CN(CC1CC1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL341897 5ht1b_human Human No 6.6 IC50 = 260 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
468 10 3 4 4.0 CNS(=O)(=O)Cc1ccc2[nH]cc(CCCN3CCC(N[C@H](C)c4ccccc4)CC3)c2c1
CHEMBL49 5ht1b_rat Rat Yes 4.6 IC50 = 26000 nM Bind
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL8412 5ht1b_rat Rat Yes 4.6 IC50 = 26000 nM Bind
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL350277 5ht1b_human Human No 6.6 IC50 = 263.0 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
361 6 2 2 3.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC(=O)NCc4ccccc4)cc32)C1
CHEMBL52612 5ht1b_rat Rat No 4.6 IC50 = 26302.7 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
318 4 0 4 3.2 c1ccc(CN2CCN(c3ncccc3-n3cccc3)CC2)cc1
CHEMBL728 5ht1b_rat Rat Yes 5.6 IC50 = 2651 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2
CHEMBL430122 5ht1b_rat Rat No 6.6 IC50 = 267 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
472 4 2 5 4.2 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(C#N)cc34)CC2)cc1N1CCN(C)CC1
CHEMBL1181152 5ht1b_rat Rat Yes 5.6 IC50 = 2690 nM Bind
Inhibition of [3H]-5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatum; Residual radioligand binding higher than 50%Inhibition of [3H]-5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatum; Residual radioligand binding higher than 50%
194 1 1 2 2.1 Clc1ccc(C2=CCNCC2)cn1
CHEMBL157110 5ht1b_rat Rat Yes 5.6 IC50 = 2690 nM Bind
Inhibition of [3H]-5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatum; Residual radioligand binding higher than 50%Inhibition of [3H]-5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatum; Residual radioligand binding higher than 50%
194 1 1 2 2.1 Clc1ccc(C2=CCNCC2)cn1
CHEMBL334923 5ht1b_human Human No 5.6 IC50 = 2691.5 nM Bind
Compound was tested for binding affinity against 5-hydroxytryptamine 1B receptorCompound was tested for binding affinity against 5-hydroxytryptamine 1B receptor
275 4 0 5 2.5 Cc1csc2c1-n1cccc1/C2=N/OCCN(C)C
CHEMBL111899 5ht1b_human Human No 7.6 IC50 = 27 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
464 9 2 6 4.0 CN(CC1CCCCC1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL115989 5ht1b_human Human No 7.6 IC50 = 27 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
422 9 2 6 2.9 CN(CC1CC1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL128 5ht1b_human Human Yes 7.6 IC50 = 27 nM Bind
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 5-hydroxytryptamine 1B receptor
295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL164111 5ht1b_human Human No 7.6 IC50 = 27 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
390 7 1 6 3.1 c1cc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)co1
CHEMBL333341 5ht1b_human Human No 7.6 IC50 = 27 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
442 9 1 5 4.5 CN(Cc1ccccc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL274866 5ht1b_rat Rat Yes 7.6 IC50 = 27 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F
CHEMBL441296 5ht1b_human Human No 6.6 IC50 = 270 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
430 9 3 6 2.9 OC[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1
CHEMBL133375 5ht1b_rat Rat No 5.6 IC50 = 2700 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
468 8 0 5 4.7 CCCN1CCCC12COc1cccc(OCCCCN3C(=O)CC4(CCCC4)CC3=O)c1C2
CHEMBL104 5ht1b_rat Rat Yes 4.6 IC50 = 27310 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1
CHEMBL435060 5ht1b_human Human No 6.6 IC50 = 275 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
387 7 1 5 3.6 c1ccc(CO[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL2368259 5ht1b_human Human No 6.6 IC50 = 275.4 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
321 5 2 3 2.0 CNS(=O)(=O)Cc1ccc2[nH]cc([C@H]3C[C@H](N(C)C)C3)c2c1
CHEMBL516 5ht1b_rat Rat Yes 5.6 IC50 = 2778 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1
CHEMBL333341 5ht1b_human Human No 7.6 IC50 = 28 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
442 9 1 5 4.5 CN(Cc1ccccc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL116092 5ht1b_human Human No 7.6 IC50 = 28 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1
CHEMBL116092 5ht1b_human Human No 7.6 IC50 = 28 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1
CHEMBL116092 5ht1b_human Human No 7.6 IC50 = 28 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1
CHEMBL143893 5ht1b_human Human No 7.6 IC50 = 28 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
428 9 2 5 4.2 c1ccc(CNCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL67684 5ht1b_human Human No 7.6 IC50 = 28 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
445 8 1 4 5.7 CC(CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL64610 5ht1b_rat Rat No 6.6 IC50 = 280 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
447 6 0 4 4.2 CN1C(=O)COc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21
CHEMBL420874 5ht1b_human Human No 6.6 IC50 = 280 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL148095 5ht1b_human Human No 6.6 IC50 = 280 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
440 7 2 5 4.4 c1ccc2c(c1)CCC2NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL65321 5ht1b_human Human No 6.6 IC50 = 280 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1cccc(F)c1
CHEMBL162899 5ht1b_human Human No 6.6 IC50 = 282 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
414 7 1 5 3.0 O=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1Cc1ccccc1
CHEMBL163376 5ht1b_human Human No 6.6 IC50 = 282 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
468 7 1 5 4.5 FC(F)(F)c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL2376484 5ht1b_rat Rat No 7.5 IC50 = 29 nM Bind
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1
CHEMBL39 5ht1b_human Human Yes 7.5 IC50 = 29 nM Bind
Displacement of radiolabeled serotonin from human 5HT1B receptorDisplacement of radiolabeled serotonin from human 5HT1B receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL3645476 5ht1b_rat Rat No 6.5 IC50 = 290 nM Bind
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
338 4 2 3 3.9 CN1CCC[C@H]1Cc1c[nH]c2ccc(/N=C(\N)c3cccs3)cc12
CHEMBL1200558 5ht1b_rat Rat Yes 5.5 IC50 = 2978 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
None None None CC[C@H](C)[C@H](N)C1=N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H]2CCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H](CCCN)NC2=O)[C@@H](C)CC)CS1
CHEMBL65824 5ht1b_human Human No 8.5 IC50 = 3.1 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
435 7 1 4 4.9 Fc1ccccc1CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL27592 5ht1b_rat Rat Yes 8.5 IC50 = 3.2 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
276 1 2 1 3.3 Brc1ccc2[nH]cc(C3=CCNCC3)c2c1
CHEMBL358072 5ht1b_human Human No 8.5 IC50 = 3.3 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
415 8 2 6 3.9 c1ccc(NCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1
CHEMBL282994 5ht1b_rat Rat Yes 8.5 IC50 = 3.3 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
232 1 2 1 3.2 Clc1ccc2[nH]cc(C3=CCNCC3)c2c1
CHEMBL283257 5ht1b_rat Rat Yes 8.5 IC50 = 3.5 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
243 2 2 3 2.5 O=[N+]([O-])c1ccc2[nH]cc(C3=CCNCC3)c2c1
CHEMBL2011570 5ht1b_rat Rat Yes 8.4 IC50 = 3.7 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.
198 1 2 1 2.5 C1=C(c2c[nH]c3ccccc23)CCNC1
CHEMBL27811 5ht1b_rat Rat Yes 8.4 IC50 = 3.7 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.
198 1 2 1 2.5 C1=C(c2c[nH]c3ccccc23)CCNC1
CHEMBL326723 5ht1b_human Human No 7.5 IC50 = 30 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
501 10 4 7 3.3 CC(=O)Nc1ccc(CNCC2(O)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL331819 5ht1b_human Human No 7.5 IC50 = 30 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
424 9 2 6 3.1 CC(C)CN(C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL1385840 5ht1b_rat Rat Yes 7.5 IC50 = 30 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12
CHEMBL116092 5ht1b_human Human No 7.5 IC50 = 30.2 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1
CHEMBL116092 5ht1b_human Human No 7.5 IC50 = 30.2 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1
CHEMBL293923 5ht1b_rat Rat Yes 6.5 IC50 = 300 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
383 5 0 6 3.0 COc1ccccc1N1CCN(CCc2ccc3c(c2)sc(=O)n3C)CC1
CHEMBL59637 5ht1b_rat Rat Yes 6.5 IC50 = 300 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
339 4 1 5 3.4 Oc1nc2ccc(CCN3CCN(c4ccccc4)CC3)cc2s1
CHEMBL61819 5ht1b_rat Rat No 6.5 IC50 = 300 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
411 7 0 6 3.8 COc1ccccc1N1CCN(CCCCc2ccc3c(c2)sc(=O)n3C)CC1
CHEMBL15909 5ht1b_rat Rat No 6.5 IC50 = 300 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
505 5 3 4 4.7 CN1CCC2(CC1)COc1ccc(NC(=O)NCCN3CCC(c4c[nH]c5cc(F)ccc45)CC3)cc12
CHEMBL143894 5ht1b_human Human No 6.5 IC50 = 300 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
456 7 3 6 3.4 O[C@H]1Cc2ccccc2C1NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL2115111 5ht1b_human Human No 6.5 IC50 = 300 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
500 8 2 5 4.9 F[C@@H]1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC[C@@H]1NCc1ccccc1C(F)(F)F
CHEMBL60318 5ht1b_rat Rat No 5.5 IC50 = 3000 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
371 4 0 5 3.1 Cn1c(=O)sc2cc(CCN3CCN(c4ccc(F)cc4)CC3)ccc21
CHEMBL27991 5ht1b_rat Rat No 5.5 IC50 = 3000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1
CHEMBL298534 5ht1b_rat Rat No 5.5 IC50 = 3000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1
CHEMBL423841 5ht1b_rat Rat No 5.5 IC50 = 3000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1
CHEMBL54089 5ht1b_rat Rat No 5.5 IC50 = 3000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1
CHEMBL305062 5ht1b_human Human No 5.5 IC50 = 3000 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
433 8 1 5 4.3 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1
CHEMBL1178932 5ht1b_rat Rat No 4.5 IC50 = 30000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL50530 5ht1b_rat Rat No 4.5 IC50 = 30000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL1183479 5ht1b_rat Rat No 4.5 IC50 = 30000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL299561 5ht1b_rat Rat No 4.5 IC50 = 30000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL26783 5ht1b_rat Rat No 4.5 IC50 = 30000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1
CHEMBL50993 5ht1b_rat Rat No 4.5 IC50 = 30000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1
CHEMBL27763 5ht1b_rat Rat No 4.5 IC50 = 30000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1
CHEMBL52438 5ht1b_rat Rat No 4.5 IC50 = 30000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1
CHEMBL1909072 5ht1b_rat Rat Yes 5.5 IC50 = 3007 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1
CHEMBL416523 5ht1b_human Human No 5.5 IC50 = 3020.0 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
414 8 1 5 3.3 COc1cccc2c1CC(CNCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL324931 5ht1b_human Human No 6.5 IC50 = 304 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
310 4 1 5 1.5 CN1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL424154 5ht1b_human Human No 6.5 IC50 = 305 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
428 9 2 5 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1)c1ccccc1
CHEMBL117249 5ht1b_human Human No 6.5 IC50 = 309 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
324 5 1 5 1.9 CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL63790 5ht1b_rat Rat No 5.5 IC50 = 3090.3 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
392 3 0 7 3.6 c1cc2c(N3CCN(Cc4ccc5c(c4)OCO5)CC3)nc3ccsc3n2c1
CHEMBL60447 5ht1b_rat Rat No 7.5 IC50 = 31 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
369 4 1 6 2.7 Cn1c(=O)sc2cc(CCN3CCN(c4ccccc4O)CC3)ccc21
CHEMBL3645475 5ht1b_rat Rat No 6.5 IC50 = 310 nM Bind
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
338 4 2 3 3.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(/N=C(\N)c3cccs3)cc12
CHEMBL324931 5ht1b_human Human No 6.5 IC50 = 310 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
310 4 1 5 1.5 CN1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL64004 5ht1b_human Human No 6.5 IC50 = 310 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1
CHEMBL194305 5ht1b_rat Rat Yes 6.5 IC50 = 310 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor in ratInhibitory activity against 5-hydroxytryptamine 1B receptor in rat
242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1
CHEMBL11265 5ht1b_rat Rat No 4.5 IC50 = 31100 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL159470 5ht1b_human Human No 6.5 IC50 = 316.2 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
347 5 2 2 3.9 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(C(=O)NCc4ccccc4)cc32)C1
CHEMBL11787 5ht1b_rat Rat No 5.5 IC50 = 3162.3 nM Bind
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
436 7 1 5 4.1 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2c(ccc3ccccc23)O1
CHEMBL299524 5ht1b_rat Rat No 4.5 IC50 = 31622.8 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
374 4 0 4 3.9 Fc1ccc(CN2CCN(Cc3nc4ccccc4n4cccc34)CC2)cc1
CHEMBL1201156 5ht1b_rat Rat Yes 5.5 IC50 = 3199 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21
CHEMBL445 5ht1b_rat Rat Yes 5.5 IC50 = 3199 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21
CHEMBL112507 5ht1b_human Human No 7.5 IC50 = 32 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
415 7 2 5 3.8 OC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL117579 5ht1b_human Human No 7.5 IC50 = 32 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
414 8 1 5 3.7 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1
CHEMBL2368256 5ht1b_human Human No 7.5 IC50 = 32.4 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
299 4 3 3 2.3 CN[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1
CHEMBL148286 5ht1b_human Human No 6.5 IC50 = 320 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
378 8 1 5 3.3 C=CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL1314789 5ht1b_rat Rat Yes 5.5 IC50 = 3235.9 nM Bind
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
356 2 0 4 4.4 CSc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2
CHEMBL273490 5ht1b_rat Rat Yes 5.5 IC50 = 3235.9 nM Bind
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
356 2 0 4 4.4 CSc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2
CHEMBL162296 5ht1b_human Human No 6.5 IC50 = 325 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
350 8 2 5 2.4 C=CCNC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1
CHEMBL117579 5ht1b_human Human No 7.5 IC50 = 33 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
414 8 1 5 3.7 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1
CHEMBL161735 5ht1b_human Human No 7.5 IC50 = 33 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
415 9 1 5 4.2 c1ccc(COC[C@@H]2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL27403 5ht1b_rat Rat Yes 6.5 IC50 = 338.8 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F
CHEMBL27403 5ht1b_rat Rat Yes 6.5 IC50 = 338.8 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F
CHEMBL65413 5ht1b_rat Rat No 4.5 IC50 = 33884.4 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4sccc4n4cccc34)CC2)cc1Cl
CHEMBL146265 5ht1b_human Human No 7.5 IC50 = 34 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
458 10 3 6 3.7 OC[C@@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL115496 5ht1b_human Human Yes 6.5 IC50 = 340 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
454 7 3 7 3.0 CC(C)(C)OC(=O)NCC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL1275709 5ht1b_human Human No 6.5 IC50 = 340 nM Bind
Binding affinity to 5HT1B receptorBinding affinity to 5HT1B receptor
253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1
CHEMBL359744 5ht1b_rat Rat Yes 4.5 IC50 = 34464 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1
CHEMBL53463 5ht1b_rat Rat Yes 4.5 IC50 = 34464 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1
CHEMBL331970 5ht1b_human Human No 7.5 IC50 = 35 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL146024 5ht1b_human Human No 7.5 IC50 = 35 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
434 8 1 6 4.3 CN(Cc1ccsc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL331970 5ht1b_human Human No 7.5 IC50 = 35 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL370110 5ht1b_human Human No 7.5 IC50 = 35 nM Funct
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1
CHEMBL146150 5ht1b_human Human No 6.5 IC50 = 350 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
485 9 3 6 4.5 CC(=O)Nc1ccc([C@@H](C)NC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL415933 5ht1b_rat Rat No 5.5 IC50 = 3548.1 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
404 7 0 7 3.3 COc1ccc2c(c1)nc(N1CCN(CCCCn3cccn3)CC1)c1cccn12
CHEMBL275481 5ht1b_human Human No 4.5 IC50 = 35481.3 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
366 5 0 4 3.6 CCCN1CCN(Cc2ccccc2)CC12COc1cccc(OC)c1C2
CHEMBL116463 5ht1b_human Human No 5.5 IC50 = 3580 nM Bind
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1
CHEMBL1626 5ht1b_rat Rat Yes 6.5 IC50 = 359 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C
CHEMBL164413 5ht1b_human Human No 7.4 IC50 = 36 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
390 7 2 6 2.2 c1c[nH]c(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)n1
CHEMBL294730 5ht1b_rat Rat No 6.4 IC50 = 360 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
397 6 0 6 3.4 COc1ccccc1N1CCN(CCCc2ccc3c(c2)sc(=O)n3C)CC1
CHEMBL304197 5ht1b_human Human No 6.4 IC50 = 360 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
416 7 2 6 2.5 OC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCN(Cc2ccccc2)CC1
CHEMBL420965 5ht1b_human Human No 7.4 IC50 = 37 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL341474 5ht1b_rat Rat Yes 6.4 IC50 = 371 nM Bind
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
284 1 0 4 2.4 CN1CCN(c2nc3cc(F)ccc3n3cccc23)CC1
CHEMBL629 5ht1b_rat Rat Yes 5.4 IC50 = 3730 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C
CHEMBL304833 5ht1b_human Human No 6.4 IC50 = 380 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1F
CHEMBL18772 5ht1b_rat Rat Yes 6.4 IC50 = 380 nM Bind
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2
CHEMBL11265 5ht1b_rat Rat No 5.4 IC50 = 3800 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL135952 5ht1b_rat Rat No 5.4 IC50 = 3800 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
410 5 0 4 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCCC12COc1ccccc1C2
CHEMBL56 5ht1b_rat Rat Yes 5.4 IC50 = 3801.9 nM Bind
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL2368260 5ht1b_human Human No 5.4 IC50 = 3801.9 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
354 4 2 3 2.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CN4C(=O)NC(C)(C)C4=O)cc32)C1
CHEMBL11265 5ht1b_human Human No 5.4 IC50 = 3801.9 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL54125 5ht1b_rat Rat No 4.4 IC50 = 38018.9 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
360 3 0 4 3.9 Fc1ccc(CN2CCN(c3nc4ccccc4n4cccc34)CC2)cc1
CHEMBL159536 5ht1b_human Human No 5.4 IC50 = 3890.5 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
309 4 2 3 3.0 Cc1nc(Cc2ccc3[nH]cc([C@H]4C[C@H](N(C)C)C4)c3c2)n[nH]1
CHEMBL164046 5ht1b_human Human No 7.4 IC50 = 39 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
428 8 2 5 4.1 CC(C)(NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1
CHEMBL161969 5ht1b_human Human No 5.4 IC50 = 3900 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
414 7 1 5 3.0 O=C1CN(Cc2ccccc2)CCN1CCCc1c[nH]c2ccc(-n3cnnc3)cc12
CHEMBL12311 5ht1b_rat Rat No 6.4 IC50 = 398.1 nM Bind
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
436 7 1 5 4.1 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccc3ccccc3c2O1
CHEMBL161045 5ht1b_human Human No 8.4 IC50 = 4.4 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
267 4 1 4 2.0 c1cc2[nH]cc(CCN3CCC3)c2cc1-n1cnnc1
CHEMBL39 5ht1b_rat Rat Yes 8.3 IC50 = 4.6 nM Bind
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht1b_rat Rat Yes 8.3 IC50 = 4.9 nM Bind
Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternolDisplacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternol
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht1b_rat Rat Yes 8.3 IC50 = 4.9 nM Bind
Displacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting methodDisplacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting method
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL347570 5ht1b_human Human No 7.4 IC50 = 40 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
513 9 2 6 4.1 CC(=O)Nc1ccc(C(=O)N(C)CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL64845 5ht1b_rat Rat No 6.4 IC50 = 400 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
435 6 1 5 5.2 Oc1nc2ccc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1
CHEMBL283207 5ht1b_rat Rat No 6.4 IC50 = 400 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1
CHEMBL52396 5ht1b_rat Rat No 6.4 IC50 = 400 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1
CHEMBL147961 5ht1b_human Human No 6.4 IC50 = 400 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cncn4)cc23)CC1)c1ccccc1
CHEMBL28287 5ht1b_rat Rat No 4.4 IC50 = 40000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL50722 5ht1b_rat Rat No 4.4 IC50 = 40000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL71 5ht1b_rat Rat Yes 5.4 IC50 = 4041 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C
CHEMBL62911 5ht1b_rat Rat No 4.4 IC50 = 40738.0 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
363 3 0 4 4.0 C[N+]1(Cc2ccccc2)CCN(c2nc3ccsc3n3cccc23)CC1
CHEMBL905 5ht1b_human Human Yes 7.4 IC50 = 41 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C
CHEMBL159759 5ht1b_human Human No 7.4 IC50 = 41 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
414 8 2 5 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1
CHEMBL148233 5ht1b_human Human No 7.4 IC50 = 41 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
406 8 1 5 4.0 CC(C)=CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL147838 5ht1b_human Human No 6.4 IC50 = 410 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
468 7 1 5 5.4 c1ccc(C2CCCCN2C2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL51118 5ht1b_rat Rat No 6.4 IC50 = 416.9 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
298 3 0 5 2.9 C=CCN1CCN(c2nc3sccc3n3cccc23)CC1
CHEMBL51118 5ht1b_rat Rat No 6.4 IC50 = 416.9 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
298 3 0 5 2.9 C=CCN1CCN(c2nc3sccc3n3cccc23)CC1
CHEMBL144002 5ht1b_human Human No 6.4 IC50 = 420 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cncn4)cc23)CC1)c1ccccc1
CHEMBL1255834 5ht1b_rat Rat Yes 6.4 IC50 = 421.1 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N
CHEMBL302431 5ht1b_rat Rat No 5.4 IC50 = 4265.8 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1Cl
CHEMBL117249 5ht1b_human Human No 6.4 IC50 = 430 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
324 5 1 5 1.9 CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL54246 5ht1b_rat Rat No 4.4 IC50 = 43651.6 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
357 3 0 5 3.5 Cc1ccnc2c1nc(N1CCN(Cc3ccccc3)CC1)c1cccn12
CHEMBL158638 5ht1b_human Human No 7.4 IC50 = 44.7 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
257 3 2 2 2.1 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(C(N)=O)cc32)C1
CHEMBL137643 5ht1b_rat Rat No 5.4 IC50 = 4400 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
219 1 1 3 1.8 COc1cccc2c1CC1(CCCN1)CO2
CHEMBL162722 5ht1b_human Human No 7.4 IC50 = 45 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
428 8 1 5 4.1 CC(CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL146335 5ht1b_human Human No 7.4 IC50 = 45 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
471 9 3 6 3.9 CC(=O)Nc1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL163114 5ht1b_human Human No 7.3 IC50 = 46 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
496 9 1 8 3.9 Cc1noc(-c2ccc(CCN3CCN(CCCc4c[nH]c5ccc(-n6cnnc6)cc45)CC3)cc2)n1
CHEMBL60047 5ht1b_rat Rat No 6.3 IC50 = 460 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
419 4 0 4 3.4 CN1C(=O)COc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21
CHEMBL146129 5ht1b_human Human No 6.3 IC50 = 460 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
476 10 4 5 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCCN4CCC(N[C@@H](CO)c5ccccc5)CC4)c3c2)CO1
CHEMBL15139 5ht1b_rat Rat No 6.3 IC50 = 467 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
423 6 4 5 3.0 COc1ccc(NC(=O)NCCc2c[nH]c3ccc(O)cc23)cc1N1CCN(C)CC1
CHEMBL294368 5ht1b_rat Rat No 5.3 IC50 = 4677.4 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)c(Cl)c1
CHEMBL326125 5ht1b_human Human No 7.3 IC50 = 47 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
444 9 3 6 3.3 OC1(CNCc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL420965 5ht1b_human Human No 7.3 IC50 = 47 nM Bind
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL420965 5ht1b_human Human No 7.3 IC50 = 47 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL159819 5ht1b_human Human No 7.3 IC50 = 47 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
400 8 2 5 3.4 c1ccc(CNC[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL420965 5ht1b_human Human No 7.3 IC50 = 47 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL116153 5ht1b_human Human No 7.3 IC50 = 47 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
450 8 1 5 3.8 Fc1cc(F)cc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL964 5ht1b_rat Rat Yes 5.3 IC50 = 4720 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC
CHEMBL349893 5ht1b_human Human No 7.3 IC50 = 48 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
401 8 2 6 2.8 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)nc1
CHEMBL143947 5ht1b_human Human No 7.3 IC50 = 48 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
458 9 3 6 3.9 C[C@@H](O)[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL275742 5ht1b_rat Rat Yes 6.3 IC50 = 489.8 nM Bind
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12
CHEMBL49932 5ht1b_rat Rat No 4.3 IC50 = 48977.9 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
387 3 0 7 2.9 c1cnc2c(c1)nc(N1CCN(Cc3ccc4c(c3)OCO4)CC1)c1cccn12
CHEMBL159483 5ht1b_human Human No 7.3 IC50 = 49 nM Bind
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
432 9 3 4 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCN4CC[C@@H](CNCc5ccccc5)C4)c3c2)CO1
CHEMBL159483 5ht1b_human Human No 7.3 IC50 = 49 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
432 9 3 4 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCN4CC[C@@H](CNCc5ccccc5)C4)c3c2)CO1
CHEMBL160070 5ht1b_human Human No 7.3 IC50 = 49 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
446 9 3 4 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(C[C@H]4COC(=O)N4)cc23)C1)c1ccccc1
CHEMBL293678 5ht1b_human Human No 7.3 IC50 = 49 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
431 8 1 4 5.1 FC1(CCc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL3645479 5ht1b_rat Rat No 6.3 IC50 = 490 nM Bind
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
324 3 2 3 3.7 CN1CCC(c2c[nH]c3ccc(/N=C(\N)c4cccs4)cc23)C1
CHEMBL39 5ht1b_human Human Yes 8.3 IC50 = 5 nM Bind
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht1b_rat Rat Yes 8.3 IC50 = 5 nM Bind
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL65765 5ht1b_human Human No 8.3 IC50 = 5.3 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
435 7 1 4 4.9 Fc1cccc(CC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL160070 5ht1b_human Human No 7.3 IC50 = 50 nM Bind
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
446 9 3 4 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(C[C@H]4COC(=O)N4)cc23)C1)c1ccccc1
CHEMBL159819 5ht1b_human Human No 7.3 IC50 = 50 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
400 8 2 5 3.4 c1ccc(CNC[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL15855 5ht1b_rat Rat No 7.3 IC50 = 50 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
447 4 2 4 4.3 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1
CHEMBL15961 5ht1b_rat Rat No 7.3 IC50 = 50 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4cccc(F)c34)CC2)cc1N1CCN(C)CC1
CHEMBL1275791 5ht1b_human Human No 6.3 IC50 = 500 nM Bind
Binding affinity to 5HT1B receptorBinding affinity to 5HT1B receptor
246 2 1 1 3.5 CN(C)[C@H]1CC[C@@H](c2c[nH]c3ccc(F)cc23)C1
CHEMBL11592 5ht1b_rat Rat Yes 5.3 IC50 = 5000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL301060 5ht1b_rat Rat Yes 5.3 IC50 = 5000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL11592 5ht1b_rat Rat Yes 5.3 IC50 = 5000 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL301060 5ht1b_rat Rat Yes 5.3 IC50 = 5000 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL439849 5ht1b_rat Rat Yes 5.3 IC50 = 5000 nM Bind
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2
CHEMBL8412 5ht1b_rat Rat Yes 4.3 IC50 = 50000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL416747 5ht1b_rat Rat No 4.3 IC50 = 50000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1
CHEMBL8412 5ht1b_rat Rat Yes 4.3 IC50 = 50000 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL12124 5ht1b_rat Rat Yes 5.3 IC50 = 5011.9 nM Bind
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNC[C@@H]1COc2ccccc2O1
CHEMBL11592 5ht1b_human Human Yes 5.3 IC50 = 5011.9 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL301060 5ht1b_human Human Yes 5.3 IC50 = 5011.9 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL274866 5ht1b_rat Rat Yes 7.3 IC50 = 51 nM Bind
Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uM
230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F
CHEMBL283606 5ht1b_rat Rat Yes 6.3 IC50 = 510 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1
CHEMBL422191 5ht1b_human Human No 5.3 IC50 = 5100 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
338 6 1 5 2.3 CN1CCN(CCCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL137486 5ht1b_rat Rat No 4.3 IC50 = 51100 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
458 8 1 5 3.9 COc1cccc2c1CC1(CCCCN1CCCCNS(=O)(=O)c1ccc(C)cc1)CO2
CHEMBL292262 5ht1b_human Human No 6.3 IC50 = 520 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
450 8 1 5 3.6 Fc1ccccc1CCN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL143510 5ht1b_human Human No 6.3 IC50 = 530 nM Bind
Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.
364 7 1 4 3.3 CCN(CC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12
CHEMBL303514 5ht1b_human Human No 6.3 IC50 = 540 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
450 8 1 5 3.6 Fc1ccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL112558 5ht1b_human Human No 7.3 IC50 = 55 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
445 9 3 7 2.7 OC1(CNCc2ccccn2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL163462 5ht1b_human Human No 7.3 IC50 = 55 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
443 8 2 6 2.5 NC(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL7257 5ht1b_human Human Yes 6.3 IC50 = 550 nM Bind
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL276175 5ht1b_rat Rat Yes 5.3 IC50 = 5530 nM Bind
compound was measured for affinity against 5-hydroxytryptamine 1B receptor labelled with [3H]5-HT radioligand in striatum tissuecompound was measured for affinity against 5-hydroxytryptamine 1B receptor labelled with [3H]5-HT radioligand in striatum tissue
442 6 0 7 3.4 O=C1CC2(CCCC2)CC(=O)N1OCCCN1CCN(c2nsc3ccccc23)CC1
CHEMBL163127 5ht1b_human Human No 7.3 IC50 = 56 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
457 8 2 6 3.5 CC(=O)Nc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL2110300 5ht1b_human Human No 6.3 IC50 = 562.3 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
313 4 2 3 2.6 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1
CHEMBL52625 5ht1b_rat Rat No 4.3 IC50 = 56234.1 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
361 3 0 5 3.3 Fc1ccc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)cc1
CHEMBL15808 5ht1b_rat Rat No 6.3 IC50 = 567 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
437 3 2 4 3.7 COc1ccc(NC(=O)N2CCc3[nH]c4ccc(F)cc4c3C2)cc1N1CCN(C)CC1
CHEMBL330803 5ht1b_human Human No 6.3 IC50 = 568 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
295 4 1 4 2.8 c1cc2[nH]cc(CCN3CCCCC3)c2cc1-n1cnnc1
CHEMBL331143 5ht1b_human Human No 7.2 IC50 = 57 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
408 9 3 6 2.5 OC1(CNCC2CC2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL2376487 5ht1b_rat Rat No 6.2 IC50 = 570 nM Bind
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1
CHEMBL330803 5ht1b_human Human No 6.2 IC50 = 570 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
295 4 1 4 2.8 c1cc2[nH]cc(CCN3CCCCC3)c2cc1-n1cnnc1
CHEMBL159381 5ht1b_human Human No 6.2 IC50 = 575 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
401 8 1 5 4.0 c1ccc(COC[C@H]2CCCN2CCc2c[nH]c3ccc(-n4cnnc4)cc23)cc1
CHEMBL159733 5ht1b_human Human No 6.2 IC50 = 575 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
428 9 1 5 3.8 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1
CHEMBL62274 5ht1b_rat Rat No 6.2 IC50 = 575.4 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
298 3 0 5 2.9 C=CCN1CCN(c2nc3ccsc3n3cccc23)CC1
CHEMBL146391 5ht1b_human Human No 7.2 IC50 = 58 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
442 9 2 5 4.7 C[C@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL133939 5ht1b_human Human No 5.2 IC50 = 5800 nM Bind
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
244 3 1 2 2.8 COc1ccc2[nH]cc(C[C@@H]3CCCN3C)c2c1
CHEMBL68019 5ht1b_human Human No 5.2 IC50 = 5800 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
449 8 1 4 5.3 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(CCc2ccccc2)CC1
CHEMBL52867 5ht1b_rat Rat No 4.2 IC50 = 58884.4 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
437 3 0 7 4.1 c1cnc2ccc3nc(N4CCN(Cc5ccc6c(c5)OCO6)CC4)c4cccn4c3c2c1
CHEMBL161696 5ht1b_human Human No 7.2 IC50 = 59 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
434 7 1 5 4.2 Clc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL159650 5ht1b_human Human No 7.2 IC50 = 59 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
428 9 1 5 4.1 CN(Cc1ccccc1)C[C@@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C1
CHEMBL18785 5ht1b_rat Rat Yes 8.2 IC50 = 6 nM Bind
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1
CHEMBL1185 5ht1b_human Human Yes 8.2 IC50 = 6.2 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C
CHEMBL147148 5ht1b_human Human No 8.2 IC50 = 6.2 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
471 8 2 5 4.6 CN(CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)C(=O)Nc1ccccc1
CHEMBL359447 5ht1b_rat Rat Yes 8.2 IC50 = 6.3 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
483 5 2 7 4.7 Cc1nnc(-c2ccc(-c3ccc(C(=O)Nc4ccc(O)c(N5CCN(C)CC5)c4)cc3)c(C)c2)o1
CHEMBL39 5ht1b_human Human Yes 8.2 IC50 = 6.5 nM Bind
Binding affinity to human 5-HT1B receptor by radioligand displacement assayBinding affinity to human 5-HT1B receptor by radioligand displacement assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL143952 5ht1b_human Human No 7.2 IC50 = 60 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
478 9 2 6 3.4 O=S(=O)(NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL151894 5ht1b_rat Rat No 7.2 IC50 = 60 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
533 7 1 8 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1
CHEMBL59741 5ht1b_rat Rat No 6.2 IC50 = 600 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
407 4 1 5 4.4 Oc1nc2ccc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1
CHEMBL11592 5ht1b_rat Rat Yes 5.2 IC50 = 6000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL301060 5ht1b_rat Rat Yes 5.2 IC50 = 6000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL11592 5ht1b_rat Rat Yes 5.2 IC50 = 6000 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL301060 5ht1b_rat Rat Yes 5.2 IC50 = 6000 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL264027 5ht1b_rat Rat No 4.2 IC50 = 60000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
306 7 1 4 1.8 CCCN(CCNC(C)=O)C1COc2cccc(OC)c2C1
CHEMBL26715 5ht1b_rat Rat No 4.2 IC50 = 60000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
306 7 1 4 1.8 CCCN(CCNC(C)=O)C1COc2cccc(OC)c2C1
CHEMBL115352 5ht1b_human Human No 7.2 IC50 = 61 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
438 8 2 6 3.5 CN(CC(C)(C)C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL292935 5ht1b_rat Rat No 7.2 IC50 = 61 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
383 6 1 6 3.8 COc1ccccc1N1CCN(CCCc2ccc3nc(O)sc3c2)CC1
CHEMBL3286557 5ht1b_human Human Yes 6.2 IC50 = 610 nM Bind
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2
CHEMBL161780 5ht1b_human Human No 7.2 IC50 = 62 nM Bind
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
440 10 3 4 2.9 CNS(=O)(=O)Cc1ccc2[nH]cc(CCN3CC[C@@H](CNCc4ccccc4)C3)c2c1
CHEMBL161780 5ht1b_human Human No 7.2 IC50 = 62 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
440 10 3 4 2.9 CNS(=O)(=O)Cc1ccc2[nH]cc(CCN3CC[C@@H](CNCc4ccccc4)C3)c2c1
CHEMBL345657 5ht1b_human Human No 7.2 IC50 = 62 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
401 8 2 6 2.8 c1cncc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)c1
CHEMBL432332 5ht1b_human Human No 7.2 IC50 = 62 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
417 7 1 4 4.6 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1
CHEMBL16035 5ht1b_rat Rat No 7.2 IC50 = 63 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
425 6 3 4 3.4 COc1ccc(NC(=O)NCCc2c[nH]c3ccc(F)cc23)cc1N1CCN(C)CC1
CHEMBL143951 5ht1b_human Human No 7.2 IC50 = 63 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
324 5 2 5 2.1 NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL12152 5ht1b_rat Rat Yes 6.2 IC50 = 631.0 nM Bind
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2O1
CHEMBL2368258 5ht1b_human Human No 5.2 IC50 = 6309.6 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
326 4 2 3 2.0 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CN4C(=O)CNC4=O)cc32)C1
CHEMBL64727 5ht1b_rat Rat No 4.2 IC50 = 63095.7 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4sccc4n4cccc34)CC2)c(Cl)c1
CHEMBL280314 5ht1b_rat Rat No 6.2 IC50 = 633 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
454 7 2 4 4.7 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)cc1OCCN(C)C
CHEMBL261977 5ht1b_rat Rat No 6.2 IC50 = 645.7 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
374 4 0 5 4.4 C(=C/c1ccccc1)\CN1CCN(c2nc3ccsc3n3cccc23)CC1
CHEMBL51 5ht1b_human Human Yes 5.2 IC50 = 6500 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2
CHEMBL147546 5ht1b_human Human No 7.2 IC50 = 66 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
499 10 2 6 4.3 CC(=O)Nc1ccc(CCN(C)C2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL343667 5ht1b_human Human No 7.2 IC50 = 66 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
520 10 1 7 3.9 CN(Cc1ccc(S(C)(=O)=O)cc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL143967 5ht1b_human Human No 6.2 IC50 = 660 nM Bind
Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.
392 9 1 4 4.1 CCCN(CCC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12
CHEMBL11265 5ht1b_human Human No 5.2 IC50 = 6606.9 nM Bind
Compound was evaluated for the binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]ketanserin.Compound was evaluated for the binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]ketanserin.
440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL293879 5ht1b_rat Rat No 6.2 IC50 = 676.1 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
344 4 0 7 2.2 CCOC(=O)CN1CCN(c2nc3ccsc3n3cccc23)CC1
CHEMBL2114036 5ht1b_human Human No 6.2 IC50 = 680 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
450 8 1 5 3.6 Fc1cccc(CCN2CCN(C[C@@H](F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL350153 5ht1b_human Human No 7.2 IC50 = 69 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
460 9 1 4 4.2 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(C[C@H]4COC(=O)N4C)cc23)C1
CHEMBL137478 5ht1b_rat Rat No 4.2 IC50 = 69100 nM Bind
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
275 3 0 3 3.3 CCCN1CCCCC12COc1cccc(OC)c1C2
CHEMBL11425 5ht1b_human Human No 5.2 IC50 = 6918.3 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
384 7 1 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2C1
CHEMBL53662 5ht1b_rat Rat No 4.2 IC50 = 69183.1 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
390 4 0 5 4.0 COc1ccc2c(c1)nc(N1CCN(Cc3ccc(F)cc3)CC1)c1cccn12
CHEMBL422504 5ht1b_rat Rat No 8.1 IC50 = 7.3 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
483 5 2 7 4.7 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc(O)c(N5CCN(C)CC5)c4)cc3)c(C)c2)no1
CHEMBL162930 5ht1b_human Human No 8.1 IC50 = 7.4 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
311 5 1 5 2.0 c1cc2[nH]cc(CCCN3CCOCC3)c2cc1-n1cnnc1
CHEMBL418499 5ht1b_rat Rat No 7.2 IC50 = 70 nM Bind
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
421 4 0 5 4.0 Cn1c(=O)sc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21
CHEMBL443762 5ht1b_rat Rat Yes 7.2 IC50 = 70 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
561 7 1 9 4.4 Cc1nnc(-c2ccc(-c3ccc(C(=O)Nc4ccc(OS(C)(=O)=O)c(N5CCN(C)CC5)c4)cc3)c(C)c2)o1
CHEMBL12028 5ht1b_rat Rat No 6.2 IC50 = 700 nM Bind
In vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membrane
459 7 1 9 3.1 COc1ccccc1N1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1
CHEMBL151695 5ht1b_rat Rat No 6.2 IC50 = 700 nM Bind
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
615 7 1 9 5.3 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc(OS(=O)(=O)C(F)(F)F)c(N5CCN(C)CC5)c4)cc3)c(C)c2)no1
CHEMBL1183429 5ht1b_rat Rat No 5.2 IC50 = 7000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2
CHEMBL296395 5ht1b_rat Rat No 5.2 IC50 = 7000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2
CHEMBL715 5ht1b_rat Rat Yes 6.2 IC50 = 707 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C
CHEMBL18772 5ht1b_rat Rat Yes 5.2 IC50 = 7079.5 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2
CHEMBL292725 5ht1b_rat Rat No 5.2 IC50 = 7079.5 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
392 3 0 7 3.6 c1cc2c(N3CCN(Cc4ccc5c(c4)OCO5)CC3)nc3sccc3n2c1
CHEMBL18772 5ht1b_rat Rat Yes 5.2 IC50 = 7079.5 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2
CHEMBL63905 5ht1b_rat Rat No 4.2 IC50 = 70794.6 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
352 2 0 5 4.0 Fc1ccc(N2CCN(c3nc4ccsc4n4cccc34)CC2)cc1
CHEMBL298649 5ht1b_rat Rat No 4.2 IC50 = 70794.6 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
375 3 0 5 3.7 Cc1ccnc2c1nc(N1CCN(Cc3ccc(F)cc3)CC1)c1cccn12
CHEMBL115444 5ht1b_human Human No 6.2 IC50 = 708 nM Bind
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1
CHEMBL342330 5ht1b_human Human No 7.2 IC50 = 71 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
458 9 2 6 3.8 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@H](CO)c1ccccc1
CHEMBL292779 5ht1b_human Human Yes 7.1 IC50 = 72 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1
CHEMBL292779 5ht1b_human Human Yes 7.1 IC50 = 72 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1
CHEMBL303997 5ht1b_human Human No 5.1 IC50 = 7200 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
451 8 1 5 4.7 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(COc2ccccc2)CC1
CHEMBL161410 5ht1b_human Human No 7.1 IC50 = 74 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
414 8 2 5 4.0 C[C@@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1
CHEMBL146991 5ht1b_human Human No 7.1 IC50 = 74 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
441 6 2 7 4.1 Oc1nc2ccccc2n1C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL63845 5ht1b_rat Rat No 5.1 IC50 = 7413.1 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
402 2 0 5 4.9 FC(F)(F)c1cccc(N2CCN(c3nc4sccc4n4cccc34)CC2)c1
CHEMBL417608 5ht1b_human Human No 5.1 IC50 = 7413.1 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
456 10 0 5 4.4 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)CC1COc2cccc(OC)c2C1
CHEMBL292779 5ht1b_human Human Yes 7.1 IC50 = 75 nM Bind
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 5-hydroxytryptamine 1B receptor
432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1
CHEMBL2376482 5ht1b_rat Rat Yes 7.1 IC50 = 75 nM Bind
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1
CHEMBL292779 5ht1b_human Human Yes 7.1 IC50 = 75 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1
CHEMBL145997 5ht1b_human Human No 7.1 IC50 = 76 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
415 8 2 6 3.3 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1
CHEMBL15837 5ht1b_rat Rat No 7.1 IC50 = 77 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
522 8 2 5 4.2 COc1ccc(NC(=O)N2CCN(CCCCc3c[nH]c4ccc(F)cc34)CC2)cc1N1CCN(C)CC1
CHEMBL50456 5ht1b_rat Rat No 4.1 IC50 = 77624.7 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
411 3 0 5 4.5 Clc1ccc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)c(Cl)c1
CHEMBL148071 5ht1b_human Human No 7.1 IC50 = 78 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
521 11 3 7 3.0 CS(=O)(=O)NC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL161970 5ht1b_human Human No 7.1 IC50 = 78 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
428 8 1 5 3.1 O=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1CCc1ccccc1
CHEMBL357408 5ht1b_human Human No 7.1 IC50 = 78 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
404 8 2 6 3.5 c1cc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)co1
CHEMBL147979 5ht1b_human Human No 7.1 IC50 = 79 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
458 10 3 6 3.7 OC[C@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL12129 5ht1b_rat Rat Yes 6.1 IC50 = 794.3 nM Bind
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNC[C@H]1COc2ccccc2O1
CHEMBL65367 5ht1b_human Human No 8.1 IC50 = 8.1 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL1403281 5ht1b_rat Rat Yes 8.1 IC50 = 8.2 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C
CHEMBL146338 5ht1b_human Human No 8.1 IC50 = 8.9 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
499 10 3 6 4.7 CC(=O)Nc1ccc([C@@H](C)NCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL147940 5ht1b_human Human No 8.1 IC50 = 8.9 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
485 10 3 6 4.1 CC(=O)Nc1ccc(CNCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL278917 5ht1b_rat Rat No 7.1 IC50 = 80 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1N1CCN(C)CC1
CHEMBL189118 5ht1b_human Human No 6.1 IC50 = 800 nM Bind
Inhibitory concentration against 5-hydroxytryptamine 1B receptorInhibitory concentration against 5-hydroxytryptamine 1B receptor
472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12
CHEMBL26018 5ht1b_rat Rat No 5.1 IC50 = 8000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL300735 5ht1b_rat Rat No 5.1 IC50 = 8000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL146396 5ht1b_human Human No 7.1 IC50 = 81 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
390 7 1 5 3.1 CC#CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL162449 5ht1b_rat Rat No 6.1 IC50 = 825 nM Bind
Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uM
247 1 0 3 2.6 COc1cc(C)cc2c1[C@H]1CCCN(C)[C@@H]1CO2
CHEMBL324751 5ht1b_human Human No 7.1 IC50 = 83 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
458 9 3 6 3.6 Cc1ccccc1CNCC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL119668 5ht1b_human Human Yes 7.1 IC50 = 83 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
450 8 1 5 3.8 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1F
CHEMBL137485 5ht1b_human Human No 6.1 IC50 = 830 nM Bind
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
244 3 1 2 2.8 COc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1
CHEMBL350637 5ht1b_human Human No 6.1 IC50 = 831.8 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
296 3 1 4 3.3 Cc1noc(-c2ccc3[nH]cc([C@H]4C[C@H](N(C)C)C4)c3c2)n1
CHEMBL113831 5ht1b_human Human No 7.1 IC50 = 85 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
424 8 3 6 3.1 CC(C)(C)CNCC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL148110 5ht1b_human Human No 7.1 IC50 = 85 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
471 9 3 6 3.8 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)C(=O)Nc1ccccc1
CHEMBL2079627 5ht1b_rat Rat No 7.1 IC50 = 85 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)cc1N1CCN(C)CC1
CHEMBL352123 5ht1b_human Human No 7.1 IC50 = 85 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
428 9 1 5 3.9 c1ccc(CCCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL326371 5ht1b_human Human No 7.1 IC50 = 85 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
401 8 1 5 3.8 c1ccc(COC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL145849 5ht1b_human Human No 7.1 IC50 = 85 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
472 10 2 6 4.1 CN(CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](CO)c1ccccc1
CHEMBL198463 5ht1b_human Human No 7.1 IC50 = 85 nM Funct
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1
CHEMBL633 5ht1b_rat Rat Yes 4.1 IC50 = 86167 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2
CHEMBL531 5ht1b_rat Rat Yes 7.1 IC50 = 87 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3
CHEMBL159493 5ht1b_human Human No 7.1 IC50 = 87 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
386 7 2 5 3.7 c1ccc(NC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL348864 5ht1b_human Human No 7.1 IC50 = 87 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
442 9 1 5 4.4 C[C@@H](c1ccccc1)N(C)C[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1
CHEMBL326371 5ht1b_human Human No 7.1 IC50 = 88 nM Bind
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
401 8 1 5 3.8 c1ccc(COC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1
CHEMBL114303 5ht1b_human Human No 7.1 IC50 = 89 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
472 9 2 6 3.9 Cc1ccccc1CN(C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL343217 5ht1b_human Human No 7.1 IC50 = 89 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
476 10 2 6 4.3 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1
CHEMBL434315 5ht1b_human Human No 7.1 IC50 = 89 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
418 8 1 6 3.9 CN(Cc1ccco1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL1550957 5ht1b_rat Rat Yes 6.1 IC50 = 890 nM Bind
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1
CHEMBL1306 5ht1b_rat Rat Yes 4.1 IC50 = 89897 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1
CHEMBL146483 5ht1b_human Human No 8.0 IC50 = 9.3 nM Bind
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
499 10 3 6 4.7 CC(=O)Nc1ccc([C@H](C)NCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1
CHEMBL163386 5ht1b_human Human No 8.0 IC50 = 9.5 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
430 8 2 6 3.0 OCC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL2368254 5ht1b_human Human No 8.0 IC50 = 9.6 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
278 3 2 2 4.2 N[C@H]1C[C@H](c2c[nH]c3ccc(Oc4ccccc4)cc32)C1
CHEMBL26018 5ht1b_rat Rat No 5.1 IC50 = 9000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL300735 5ht1b_rat Rat No 5.1 IC50 = 9000 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL65710 5ht1b_rat Rat No 4.0 IC50 = 91201.1 nM Bind
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
348 3 0 5 3.9 c1ccc(CN2CCN(c3nc4sccc4n4cccc34)CC2)cc1
CHEMBL351311 5ht1b_human Human No 7.0 IC50 = 93 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
415 8 1 6 2.9 c1cncc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1
CHEMBL159627 5ht1b_human Human No 7.0 IC50 = 93 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
311 5 2 5 1.6 OC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1
CHEMBL349528 5ht1b_human Human No 7.0 IC50 = 93 nM Bind
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
297 4 2 5 1.4 O[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1
CHEMBL304993 5ht1b_human Human No 6.0 IC50 = 930 nM Bind
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
432 8 1 5 3.5 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCN(CCc2ccccc2)CC1
CHEMBL148087 5ht1b_human Human No 7.0 IC50 = 95 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
428 8 2 5 4.5 C[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL114877 5ht1b_human Human No 7.0 IC50 = 96 nM Bind
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
458 9 2 6 3.6 CN(Cc1ccccc1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL2368253 5ht1b_human Human No 7.0 IC50 = 97.7 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
306 4 1 2 4.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(Oc4ccccc4)cc32)C1
CHEMBL2368257 5ht1b_human Human No 7.0 IC50 = 97.7 nM Bind
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
327 4 1 3 3.0 CN1C(=O)OCC1Cc1ccc2[nH]cc([C@H]3C[C@H](N(C)C)C3)c2c1
CHEMBL50740 5ht1b_rat Rat No 4.0 IC50 = 97723.7 nM Bind
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
393 3 0 5 4.4 c1ccc(CN2CCN(c3nc4ccc5ncccc5c4n4cccc34)CC2)cc1
CHEMBL148194 5ht1b_human Human No 7.0 IC50 = 98 nM Bind
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
458 9 3 6 3.6 CC(CO)(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1
CHEMBL143767 5ht1b_human Human No 7.0 IC50 = 98 nM Bind
Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.
336 5 1 4 2.5 CN(C)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12
CHEMBL116031 5ht1b_human Human No 7.0 IC50 = 98 nM Bind
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
432 8 1 5 3.7 Fc1ccccc1CCN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1
CHEMBL119668 5ht1b_human Human Yes 7.0 IC50 = 98 nM Bind
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
450 8 1 5 3.8 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1F
CHEMBL1241913 5ht1b_human Human Yes 8.9 Kd = 1.2 nM Funct
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1
CHEMBL1185 5ht1b_human Human Yes 8.8 Kd = 1.5 nM Bind
Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.
287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C
CHEMBL275507 5ht1b_human Human Yes 4.9 Kd = 14125.4 nM Funct
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1
CHEMBL1181270 5ht1b_human Human No 5.7 Kd = 1862.1 nM Funct
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
298 2 1 3 3.2 CC(C)n1cc2c3c(cccc31)[C@H]1C[C@@H](CO)CN(C)[C@@H]1C2
CHEMBL161046 5ht1b_human Human No 5.7 Kd = 1862.1 nM Funct
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
298 2 1 3 3.2 CC(C)n1cc2c3c(cccc31)[C@H]1C[C@@H](CO)CN(C)[C@@H]1C2
CHEMBL1181275 5ht1b_human Human No 6.7 Kd = 208.9 nM Funct
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)C1=C[C@@H](CO)CN(C)[C@@H]1C2
CHEMBL161368 5ht1b_human Human No 6.7 Kd = 208.9 nM Funct
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)C1=C[C@@H](CO)CN(C)[C@@H]1C2
CHEMBL275035 5ht1b_human Human No 5.1 Kd = 8128.3 nM Funct
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1
CHEMBL1184450 5ht1b_human Human No 6.1 Kd = 851.1 nM Funct
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)[C@H]1C=C(CO)CN(C)[C@@H]1C2
CHEMBL349405 5ht1b_human Human No 6.1 Kd = 851.1 nM Funct
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)[C@H]1C=C(CO)CN(C)[C@@H]1C2
CHEMBL442 5ht1b_rat Rat Yes 10.0 Ki = 0.1 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL144030 5ht1b_human Human No 10.0 Ki = 0.1 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12
CHEMBL144030 5ht1b_human Human No 10.0 Ki = 0.1 nM Bind
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12
CHEMBL374973 5ht1b_human Human No 10.0 Ki = 0.1 nM Bind
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
666 16 4 4 9.1 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1
CHEMBL438619 5ht1b_human Human No 10.0 Ki = 0.1 nM Funct
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccncc56)CC4)c(=O)c23)C1
CHEMBL147851 5ht1b_human Human No 10.0 Ki = 0.1 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
504 11 4 6 2.3 NCCc1c[nH]c2ccc(OCCN3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12
CHEMBL357478 5ht1b_human Human No 9.9 Ki = 0.1 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
609 12 5 7 3.4 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(N4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)cc3)cc12
CHEMBL15928 5ht1b_human Human Yes 9.9 Ki = 0.1 nM Bind
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C
CHEMBL15928 5ht1b_human Human Yes 9.9 Ki = 0.1 nM Bind
Affinity towards cloned human 5-hydroxytryptamine 1B receptorAffinity towards cloned human 5-hydroxytryptamine 1B receptor
497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C
CHEMBL339308 5ht1b_human Human No 9.9 Ki = 0.1 nM Bind
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
499 6 2 7 4.3 COc1ccc(NC(=O)c2ccc(-c3ccc(C4=NC(C)ON4)cc3C)cc2)cc1N1CCN(C)CC1
CHEMBL147901 5ht1b_human Human No 9.8 Ki = 0.2 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
435 11 5 5 2.2 NCCc1c[nH]c2ccc(OCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12
CHEMBL247428 5ht1b_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
464 6 0 6 3.2 Cc1ccc2c(OCCN3CCN(Cc4cc(F)c5c(c4)N(C)C(=O)CO5)CC3)cccc2n1
CHEMBL490417 5ht1b_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1
CHEMBL147677 5ht1b_human Human No 9.7 Ki = 0.2 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
464 12 6 5 2.4 NCCc1c[nH]c2ccc(OCCNC(=O)NCCOc3ccc4[nH]cc(CCN)c4c3)cc12
CHEMBL344127 5ht1b_human Human Yes 9.7 Ki = 0.2 nM Bind
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
377 8 2 3 3.6 COc1ccc(CNC(=O)/C=C/c2ccc3[nH]cc(CCN(C)C)c3c2)cc1
CHEMBL2112662 5ht1b_human Human No 9.7 Ki = 0.2 nM Bind
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
472 6 0 5 3.6 Cc1ccccc1CN1CCN(C(=O)COc2ccc3cccc(N4CCN(C)CC4)c3c2)CC1
CHEMBL357830 5ht1b_human Human No 9.7 Ki = 0.2 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
600 11 4 6 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCC(C4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)CC3)cc12
CHEMBL199088 5ht1b_human Human No 9.6 Ki = 0.3 nM Bind
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
441 2 0 5 3.6 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccc(C(F)(F)F)nc2)CC4)CC1
CHEMBL144128 5ht1b_human Human No 9.6 Ki = 0.3 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
490 12 4 6 2.7 NCCc1c[nH]c2ccc(OCCN3CCN(CCOc4ccc5[nH]cc(CCN)c5c4)CC3)cc12
CHEMBL356277 5ht1b_human Human No 9.6 Ki = 0.3 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
540 12 6 6 3.7 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(NC(=O)COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12
CHEMBL3647266 5ht1b_crigr Chinese hamster No 9.6 Ki = 0.3 nM Bind
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
544 7 1 7 4.6 O=C(NC1CCN(c2ncccc2Cl)CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1
CHEMBL144397 5ht1b_human Human No 9.5 Ki = 0.3 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
506 14 6 6 1.7 NCCc1c[nH]c2ccc(OCC(=O)NCCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12
CHEMBL762 5ht1b_human Human Yes 9.5 Ki = 0.3 nM Bind
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL199443 5ht1b_human Human No 9.5 Ki = 0.3 nM Funct
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cccnc56)CC4)c(=O)c23)C1
CHEMBL340786 5ht1b_human Human No 9.5 Ki = 0.3 nM Bind
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
458 5 0 5 3.6 Cc1ccccc1N1CCN(C(=O)COc2ccc3cccc(N4CCN(C)CC4)c3c2)CC1
CHEMBL473186 5ht1b_human Human Yes 9.5 Ki = 0.3 nM Bind
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C
CHEMBL484059 5ht1b_human Human No 9.5 Ki = 0.3 nM Bind
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
464 5 1 5 4.6 O=C1COc2ccc(CCN3CCN(c4cccc5nc(-c6ccccc6)ccc45)CC3)cc2N1
CHEMBL370852 5ht1b_human Human No 9.5 Ki = 0.3 nM Bind
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
406 2 0 4 3.8 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccc(Cl)cc2)CC4)CC1
CHEMBL148022 5ht1b_human Human No 9.5 Ki = 0.3 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3cccc(COc4ccc5[nH]cc(CCN)c5c4)c3)cc12
CHEMBL146720 5ht1b_human Human No 9.4 Ki = 0.4 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
518 10 4 6 1.8 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12
CHEMBL342323 5ht1b_human Human No 9.4 Ki = 0.4 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
828 25 6 8 7.2 NCCc1c[nH]c2ccc(OCCCCCCNS(=O)(=O)c3ccc(-c4ccc(S(=O)(=O)NCCCCCCOc5ccc6[nH]cc(CCN)c6c5)cc4)cc3)cc12
CHEMBL2112660 5ht1b_human Human No 9.4 Ki = 0.4 nM Bind
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
469 5 0 6 3.2 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5ccccc5C#N)CC4)cc23)CC1
CHEMBL1732 5ht1b_rat Rat Yes 9.4 Ki = 0.4 nM Bind
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL444398 5ht1b_human Human No 9.4 Ki = 0.4 nM Bind
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
390 4 2 4 3.2 Cc1cc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2[nH]1
CHEMBL496520 5ht1b_human Human No 9.4 Ki = 0.4 nM Bind
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4ccc5c(c4F)NC(=O)CO5)CC3)cccc2n1
CHEMBL197344 5ht1b_human Human No 9.4 Ki = 0.4 nM Funct
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
465 4 0 8 3.5 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccsc56)CC4)c(=O)c23)C1
CHEMBL605785 5ht1b_human Human No 9.4 Ki = 0.4 nM Bind
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
506 5 1 8 4.2 COC1(c2ccc(NC(=O)c3cc(=O)c4cc(F)cc(-c5c(C)nn(C)c5C)c4o3)cn2)CCOCC1
CHEMBL605785 5ht1b_human Human No 9.4 Ki = 0.4 nM Bind
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
506 5 1 8 4.2 COC1(c2ccc(NC(=O)c3cc(=O)c4cc(F)cc(-c5c(C)nn(C)c5C)c4o3)cn2)CCOCC1
CHEMBL129813 5ht1b_human Human No 9.4 Ki = 0.4 nM Bind
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
502 5 0 7 3.1 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6c5OCCO6)CC4)cc23)CC1
CHEMBL2112661 5ht1b_human Human No 9.4 Ki = 0.4 nM Bind
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
494 5 0 5 4.5 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6ccccc56)CC4)cc23)CC1
CHEMBL338015 5ht1b_human Human No 9.4 Ki = 0.4 nM Bind
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
504 7 0 7 3.3 COc1cccc(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c1OC
CHEMBL3650029 5ht1b_crigr Chinese hamster No 9.3 Ki = 0.5 nM Bind
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
483 7 0 7 3.5 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CC(Oc2cccnc2)C1
CHEMBL424128 5ht1b_human Human No 9.3 Ki = 0.5 nM Funct
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
434 13 4 4 4.7 NCCc1c[nH]c2ccc(OCCCCCCOc3ccc4[nH]cc(CCN)c4c3)cc12
CHEMBL1183948 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
463 4 1 5 3.7 COc1ccc(NC(=O)N2CCN(c3cccc4c3CCCC4)CC2)cc1N1CCN(C)CC1
CHEMBL325359 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
463 4 1 5 3.7 COc1ccc(NC(=O)N2CCN(c3cccc4c3CCCC4)CC2)cc1N1CCN(C)CC1
CHEMBL502138 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
680 17 4 4 9.5 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1
CHEMBL196914 5ht1b_human Human No 9.3 Ki = 0.5 nM Funct
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
473 5 0 8 2.9 COc1c(Cl)cccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1
CHEMBL198836 5ht1b_human Human No 9.3 Ki = 0.5 nM Funct
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
459 4 0 7 3.4 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccccc56)CC4)c(=O)c23)C1
CHEMBL200315 5ht1b_human Human No 9.3 Ki = 0.5 nM Funct
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
451 4 0 8 2.2 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6c5OCC6)CC4)c(=O)c23)C1
CHEMBL371221 5ht1b_human Human No 9.3 Ki = 0.5 nM Funct
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5nccc6ccccc56)CC4)c(=O)c23)C1
CHEMBL1242081 5ht1b_human Human No 9.3 Ki = 0.5 nM Funct
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
508 6 1 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CC6)ncn4-5)CC3)cccc2n1
CHEMBL282229 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
512 8 0 7 5.2 COc1cc2c(cc1OCCN(C)C)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2
CHEMBL1631532 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
404 5 1 5 4.1 COC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1
CHEMBL1632206 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
388 5 1 4 3.9 CC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1
CHEMBL490417 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1
CHEMBL497980 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
436 4 1 5 3.9 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)ccc(Cl)c2n1
CHEMBL521506 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
436 4 1 5 3.9 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1
CHEMBL522257 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1
CHEMBL490417 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1
CHEMBL194647 5ht1b_human Human No 9.3 Ki = 0.5 nM Bind
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
397 2 0 5 3.1 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccc(C#N)cc2)CC4)CC1
CHEMBL3647261 5ht1b_crigr Chinese hamster No 9.3 Ki = 0.5 nM Bind
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
509 7 1 6 4.6 O=C(NC1CCN(c2ccccc2)CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1
CHEMBL3647282 5ht1b_crigr Chinese hamster No 9.3 Ki = 0.6 nM Bind
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
540 8 1 8 4.0 COc1cccnc1N1CCC(NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)CC1
CHEMBL500284 5ht1b_human Human No 9.2 Ki = 0.6 nM Bind
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
694 18 4 4 9.9 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1
CHEMBL1241824 5ht1b_human Human No 9.2 Ki = 0.6 nM Funct
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
496 5 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N(C)C)ncn4-5)CC3)cccc2n1
CHEMBL1242167 5ht1b_human Human No 9.2 Ki = 0.6 nM Funct
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
522 6 1 7 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCC6)ncn4-5)CC3)cccc2n1
CHEMBL1290486 5ht1b_human Human No 9.2 Ki = 0.6 nM Funct
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
400 4 1 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4CCC(=O)N5)CC3)cccc2n1
CHEMBL196848 5ht1b_human Human No 9.2 Ki = 0.6 nM Bind
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
469 4 0 4 5.4 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3ccccc3C)cc1)CC2
CHEMBL484260 5ht1b_human Human No 9.2 Ki = 0.6 nM Bind
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
416 4 1 5 3.5 Cc1cc(N2CCN(CCc3ccc4c(c3)NC(=O)CO4)CC2)c2ccc(C)nc2c1
CHEMBL489195 5ht1b_human Human No 9.2 Ki = 0.6 nM Bind
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
403 4 1 6 2.6 Cc1ncc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1
CHEMBL491839 5ht1b_human Human No 9.2 Ki = 0.6 nM Bind
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
407 4 1 5 3.1 CC1(C)Cc2cccc(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)c2O1
CHEMBL198975 5ht1b_human Human No 9.2 Ki = 0.6 nM Bind
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
452 3 0 6 3.7 Cc1c(C(=O)N2CCc3cc4ccnc(N5CCN(C)CC5)c4cc32)cnn1-c1ccccc1
CHEMBL158941 5ht1b_human Human No 9.2 Ki = 0.6 nM Bind
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
692 16 2 6 4.8 CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N(C)Cc3ccc(CN(C)S(=O)(=O)Cc4ccc5[nH]cc(CCN(C)C)c5c4)cc3)cc12
CHEMBL158941 5ht1b_human Human No 9.2 Ki = 0.6 nM Bind
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
692 16 2 6 4.8 CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N(C)Cc3ccc(CN(C)S(=O)(=O)Cc4ccc5[nH]cc(CCN(C)C)c5c4)cc3)cc12
CHEMBL282950 5ht1b_human Human No 9.2 Ki = 0.7 nM Bind
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
606 11 4 7 4.6 CN1CCN(c2cccc3ccc(OCC(=O)Nc4ccc(NC(=O)COc5ccc6[nH]cc(CCN)c6c5)cc4)cc23)CC1
CHEMBL3647276 5ht1b_crigr Chinese hamster No 9.2 Ki = 0.7 nM Bind
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
484 9 1 6 4.2 COc1cccc(CCNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1
CHEMBL31217 5ht1b_human Human No 9.1 Ki = 0.8 nM Bind
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
444 8 2 5 4.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5[nH]cc(CCN)c5c4)cc23)CC1
CHEMBL31217 5ht1b_human Human No 9.1 Ki = 0.8 nM Bind
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
444 8 2 5 4.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5[nH]cc(CCN)c5c4)cc23)CC1
CHEMBL444404 5ht1b_human Human No 9.1 Ki = 0.8 nM Bind
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
554 8 4 4 6.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1
CHEMBL452387 5ht1b_human Human No 9.1 Ki = 0.8 nM Bind
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
624 13 4 4 8.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1
CHEMBL1241738 5ht1b_human Human No 9.1 Ki = 0.8 nM Funct
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnc(C)n4-5)CC3)cccc2n1
CHEMBL1289394 5ht1b_human Human No 9.1 Ki = 0.8 nM Funct
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
444 4 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@H](C)C3)cc(F)cc2n1
CHEMBL1290487 5ht1b_human Human No 9.1 Ki = 0.8 nM Funct
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
414 4 0 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4CCC(=O)N5C)CC3)cccc2n1