Mutant Browser

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Protein name Generic number Position Segment Mutation FoldChange or Qual Exp Type Ligand Reference Review
p2y12_human 3.29x29 101 TM3 S => A 1.585↑ pIC50 (CRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2009)
p2y12_human 3.29x29 101 TM3 S => A 2.513↓ pK(d) (CRE-luciferase) PSB-0739 Hoffmann K et al (2009)
p2y12_human 3.29x29 101 TM3 S => A 1.259↑ pK(b) (CRE-luciferase) Reactive red Hoffmann K et al (2009)
p2y12_human 3.29x29 101 TM3 S => A 1.0 pK(b) (CRE-luciferase) suramin Hoffmann K et al (2009)
p2y12_human 3.29x29 101 TM3 S => A 1.995↑ pK(b) (CRE-luciferase) BAY-9421 Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 3.984↓ pIC50 (CRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 6.329↓ pK(b) (CRE-luciferase) Reactive Blue 2 Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 3.984↓ pK(b) (CRE-luciferase) Reactive Blue 2 Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 31.25↓ pK(b) (CRE-luciferase) Cibacron blue 3GA Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 12.658↓ pK(b) (CRE-luciferase) MG 38-1 Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 5.0↓ pK(d) (CRE-luciferase) PSB-0739 Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 5.0↓ pK(b) (CRE-luciferase) PSB-0801 Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 1.259↓ pK(b) (CRE-luciferase) PSB-0826 Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 1.0 pK(b) (CRE-luciferase) Reactive red 2 Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 1.996↓ pK(b) (CRE-luciferase) suramin Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 1.0 pK(b) (CRE-luciferase) BAY-9421 Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 1.259↓ pK(b) (CRE-luciferase) cangrelor Hoffmann K et al (2009)
p2y12_human 3.29x29 101 TM3 S => A 1.549↑ pK(b) (cAMP accumulation) ticagrelor Hoffmann K et al (2014)
p2y12_human 5.43x43 194 TM5 C => A 2.404↓ EC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2014)
p2y12_human 5.43x43 194 TM5 C => A 2.174↓ EC50 (CRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2014)
p2y12_human 5.43x43 194 TM5 C => A 6.757↓ pK(b) (CRE-luciferase) ticagrelor Hoffmann K et al (2014)
p2y12_human 5.43x43 194 TM5 C => A 3.631↑ pK(b) (CRE-luciferase) Reactive Blue 2 Hoffmann K et al (2014)
p2y12_human 5.43x43 194 TM5 C => A 14.454↑ pK(b) (CRE-luciferase) PSB-0739 Hoffmann K et al (2014)
p2y12_human 6.47x47 248 TM6 C => A 1.096↓ pK(b) (cAMP accumulation) ticagrelor Hoffmann K et al (2014)
p2y12_human 6.55x55 256 TM6 R => A 9.009↓ EC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2014)
p2y12_human 6.55x55 256 TM6 R => A 1.122↑ pK(b) (cAMP accumulation) ticagrelor Hoffmann K et al (2014)
p2y12_human 3.29x29 101 TM3 S => A 3.984↓ pIC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 3.29x29 101 TM3 S => A 1.259↓ pK(b) (cAMP accumulation) cangrelor Hoffmann K et al (2008)
p2y12_human 3.29x29 101 TM3 S => A 1.75↑ IC50 (CRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 3.29x29 101 TM3 S => A 1.207↑ EC50 (SRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 3.29x29 101 TM3 S => A 1.585↑ pK(b) (CRE-luciferase) Reactive Blue 2 Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => K 1.585↑ pIC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => K 1.996↓ pK(b) (cAMP accumulation) cangrelor Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 76.923↓ pIC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 1.0 pK(b) (cAMP accumulation) cangrelor Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 6.41↓ IC50 (CRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 1.77↓ EC50 (SRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 7.937↓ pK(b) (cAMP accumulation) Reactive Blue 2 Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 31.25↓ pK(b) (CRE-luciferase) Reactive Blue 2 Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => D 500.0↓ pIC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2008)
Protein name Generic number Segment Position Mutation FoldChange or Qual Exp Type Ligand Reference Review


Residue

Diagrams

ICL1 R S K ICL1ECL1 L G T ECL1ICL2 P F K T S N P K ICL2ECL2 N R Q P R D K N V K K C S F L K S ECL2ICL3 R G V G K V ICL3ECL3 D V F ECL3N-term M Q A V D N L T S A P G N T S L C T R D N-termC-term L K C P N S A T S L S Q D N R K K E Q D G G D P N E E T P M C-term Y K I T Q V L F P L L Y T V L F F V G L I T N G L A M R I F F Q I S N F I I F L K N T V I S D L L M I L T F P F K I L S D A K G P L R T F V C Q V T S V I F Y F T M Y I S I S F L G L I T I D R Y Q K T T R N L L G A K I L S V V I W A F M F L L S L P N M I L T E F G L V W H E I V N Y I C Q V I F W I N F L I V I V C Y T L I T K E L Y R S Y V R T P R K K V N V K V F I I I A V F F I C F V P F H F A R I P Y T L S Q T R D C T A E N T L F Y V K E S T L W L T S L N A C L D P F I Y F F L C K S L I S F R N S M
Download: PNG | SVG Increased binding/potency: >5-fold, >10-fold; Reduced binding/potency: >5-fold, >10-fold; No/low effect (<5-fold); and N/A
G N T I L G V F F L V T Y L L P F L V Q 1 K N T V I S D L L M I L T F P F K I L S 2 L G L F S I S I Y M T F Y F I V S T V Q 3 A K I L S V V I W A F M F L L S L P N M 4 Y C V I V I L F N I W F I V Q C I Y N V 5 V F I I I A V F I F C F V P F H F A R I P 6 F P D L C A N L S T L W L T S E K V Y 7
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Residue Table


GPCRdb(A)
GPCRdb(A)
P2Y12 receptor
TM3
3x29 3.29x29 S101
TM5
5x43 5.43x43 C194
TM6
6x47 6.47x47 C248
6x55 6.55x55 R256