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Ligand source activities (1 row/activity)

Affinity
Potency

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

α-ergocryptine	358	None	18	Rat	Binding	Ki	=	5.02	8.30	-5	21	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	ChEMBL	575.3	5	3	6	2.43	CC(C)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	-
α-ergocryptine	358	None	18	Rat	Binding	pKi	=	8.30	8.08	-5	21	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	Drug Central	575.3	5	3	6	2.43	CC(C)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	-
α-ergocryptine	358	None	18	Rat	Binding	IC50	=	8.20	8.09	-5	21	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	ChEMBL	575.3	5	3	6	2.43	CC(C)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	-
α-methyl-5-HT	364	None	24	Human	Binding	Ki	=	250.00	6.60	-33	19	Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta	ChEMBL	190.1	2	3	2	1.76	CC(N)Cc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1021/jm950498t
α-methyl-5-HT	364	None	24	Rat	Binding	Ki	=	1000.00	6.00	-57	19	Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.	ChEMBL	190.1	2	3	2	1.76	CC(N)Cc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1021/jm00384a001
α-methyl-5-HT	364	None	24	Rat	Binding	Ki	=	85.00	7.07	-57	19	Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.	ChEMBL	190.1	2	3	2	1.76	CC(N)Cc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1021/jm00164a046
α-methyl-5-HT	364	125I-CYP	24	Rat	Binding	pKi	=	1000.00	6.00	-57	19	-	PDSP KiDatabase	190.1	2	3	2	1.76	CC(N)Cc1c[nH]c2ccc(O)cc12	-
α-methyl-5-HT	364	125I-CYP	24	Rat	Binding	pKi	=	1000.00	6.00	-57	19	-	PDSP KiDatabase	190.1	2	3	2	1.76	CC(N)Cc1c[nH]c2ccc(O)cc12	-
(+)-WAY 100135	4070	None	6	Human	Binding	pKi	None	-	5.80	-1258	5	Unclassified	Guide to Pharmacology	395.3	6	1	4	3.52	COc1ccccc1N1CCN(C[C@@H](C(=O)NC(C)(C)C)c2ccccc2)CC1	https://pubmed.ncbi.nlm.nih.gov/9208142
(-)-pindolol	3126	3H-5HT	37	Rat	Binding	pKi	=	77.60	7.11	-95	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-pindolol	3126	125I-CYP	37	Rat	Binding	pKi	=	64.60	7.19	-95	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-pindolol	3126	125I-ICYP	37	Rat	Binding	pKi	=	24.00	7.62	-95	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-pindolol	3126	3H-GR-125743	37	Rat	Binding	pKi	=	25.12	7.60	-95	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-pindolol	3126	None	37	Mouse	Binding	pKi	None	-	8.10	-18	15	Unclassified	Guide to Pharmacology	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	https://pubmed.ncbi.nlm.nih.gov/1557407
(-)-pindolol	3126	3H-GR-125743	37	Guinea pig	Binding	pKi	=	1479.11	5.83	-3388	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-propranolol	3187	3H-5HT	44	Human	Binding	pKi	=	2691.53	5.57	-1174	34	-	PDSP KiDatabase	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	-
(-)-propranolol	3187	3H-5HT	44	Human	Binding	pKi	=	10000.00	5.00	-1174	34	-	PDSP KiDatabase	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	-
(-)-propranolol	3187	3H-5HT	44	Human	Binding	pKi	=	630.95	6.20	-1174	34	-	PDSP KiDatabase	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	-
(-)-propranolol	3187	3H-5HT	44	Human	Binding	pKi	=	10000.00	5.00	-1174	34	-	PDSP KiDatabase	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	-
(-)-propranolol	3187	None	44	Human	Binding	pKi	=	6.20	8.21	-1174	34	None	Drug Central	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	-

Showing 1 to 20 of 2,728 entries

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

(-)-propranolol	3187	None	44	Human	Functional	Ki	=	4100.00	5.39	-	34	Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptor	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm970507t
5-HT-moduline	138	None	0	Human	Functional	pIC50	None	-	11.90	-1	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9774213
5-hydroxytryptamine	139	None	45	Human	Functional	Ki	=	6.76	8.17	-19	61	Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells	ChEMBL	176.1	2	3	2	1.38	NCCc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1021/jm960552l
5-hydroxytryptamine	139	None	45	Human	Functional	EC50	=	4.82	8.32	-19	61	Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells	ChEMBL	176.1	2	3	2	1.38	NCCc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1021/jm960552l
5-hydroxytryptamine	139	None	45	Human	Functional	EC50	=	4.67	8.33	-19	61	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 Agonist	ChEMBL	176.1	2	3	2	1.38	NCCc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1016/s0960-894x(98)00222-4
8-OH-DPAT	187	None	44	Human	Functional	EC50	=	260.00	6.58	-95	46	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	ChEMBL	247.2	5	1	2	3.37	CCCN(CCC)C1CCc2cccc(O)c2C1	https://dx.doi.org/10.1016/s0960-894x(98)00222-4
8-OH-DPAT	187	None	44	Human	Functional	pIC50	=	-	6.20	-95	46	Unclassified	Guide to Pharmacology	247.2	5	1	2	3.37	CCCN(CCC)C1CCc2cccc(O)c2C1	https://pubmed.ncbi.nlm.nih.gov/9303569
CHEMBL1181270	11722	None	0	Human	Functional	Kd	=	1862.09	5.73	-	1	Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery	ChEMBL	298.2	2	1	3	3.17	CC(C)n1cc2c3c(cccc31)[C@H]1C[C@@H](CO)CN(C)[C@@H]1C2	https://dx.doi.org/10.1021/jm981092u
CHEMBL1181275	11725	None	0	Human	Functional	Kd	=	208.93	6.68	-	1	Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery	ChEMBL	296.2	2	1	3	3.08	CC(C)n1cc2c3c(cccc31)C1=C[C@@H](CO)CN(C)[C@@H]1C2	https://dx.doi.org/10.1021/jm981092u
CHEMBL1184450	12237	None	0	Human	Functional	Kd	=	851.14	6.07	-	1	Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery	ChEMBL	296.2	2	1	3	3.10	CC(C)n1cc2c3c(cccc31)[C@H]1C=C(CO)CN(C)[C@@H]1C2	https://dx.doi.org/10.1021/jm981092u
CHEMBL120055	14430	None	0	Human	Functional	EC50	=	2.10	8.68	-3	3	The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonist	ChEMBL	392.2	6	2	4	2.71	Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1	https://dx.doi.org/10.1016/S0960-894X(97)10164-0
CHEMBL1241546	16632	None	0	Human	Functional	Ki	=	2.51	8.60	-	3	Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	440.2	4	0	7	3.69	Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C)nnn4-5)CC3)cccc2n1	https://dx.doi.org/10.1021/jm100482n
CHEMBL1241547	16633	None	0	Human	Functional	Ki	=	1.58	8.80	-	3	Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	439.2	4	0	6	4.29	Cc1cn2c(n1)COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2	https://dx.doi.org/10.1021/jm100482n
CHEMBL1241548	16634	None	0	Human	Functional	Ki	=	2.00	8.70	-	3	Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	453.3	4	0	6	4.60	Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C)c(C)n4-5)CC3)cccc2n1	https://dx.doi.org/10.1021/jm100482n
CHEMBL1241639	16638	None	0	Human	Functional	Ki	=	7.94	8.10	-	3	Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	427.2	4	0	8	2.78	Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnnn4-5)CC3)cccc2n1	https://dx.doi.org/10.1021/jm100482n
CHEMBL1241640	16639	None	0	Human	Functional	Ki	=	1.26	8.90	-	3	Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	497.2	6	0	8	4.16	CCOC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2	https://dx.doi.org/10.1021/jm100482n
CHEMBL1241641	16640	None	0	Human	Functional	Ki	=	1.00	9.00	-	3	Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	493.2	4	0	6	5.00	Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C(F)(F)F)cn4-5)CC3)cccc2n1	https://dx.doi.org/10.1021/jm100482n
CHEMBL1241642	16641	None	0	Human	Functional	Ki	=	1.00	9.00	-	3	Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	425.2	4	0	6	3.99	Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4cncn4-5)CC3)cccc2n1	https://dx.doi.org/10.1021/jm100482n
CHEMBL1241736	16643	None	0	Human	Functional	Ki	=	1.00	9.00	-	3	Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	467.2	5	0	7	4.19	CC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2	https://dx.doi.org/10.1021/jm100482n
CHEMBL1241737	16644	None	0	Human	Functional	Ki	=	2.51	8.60	-	3	Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	496.3	6	0	8	4.36	CO/N=C(\C)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2	https://dx.doi.org/10.1021/jm100482n

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Ligand source activities (1 row/activity)