Mutant Browser

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Protein name Generic number Position Segment Mutation FoldChange or Qual Exp Type Ligand Reference Review
Protein name Generic number Segment Position Mutation FoldChange or Qual Exp Type Ligand Reference Review
p2y12_human 6.55x55 256 TM6 R => A 1.259↓ pK(b) (CRE-luciferase) Cangrelor Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 6.31↓ pK(b) (CRE-luciferase) Reactive blue 2 meta Hoffmann K et al (2009)
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 1.206↑ EC50 (SRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 1.0 pK(b) (CRE-luciferase) Reactive red 2 Hoffmann K et al (2009)
p2y12_human 3.29x29 101 TM3 S => A 1.751↑ IC50 (CRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 3.29x29 101 TM3 S => A 1.996↑ pK(b) (CRE-luciferase) BAY-9421 Hoffmann K et al (2009)
p2y12_human 5.43x43 194 TM5 C => A 2.173↓ EC50 (CRE-luciferase) 2-methylthio-ADP 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 5.43x43 194 TM5 C => A 2.404↓ EC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2014)
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 9.038↓ EC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2014)
p2y12_human 6.55x55 256 TM6 R => A 31.623↓ pK(b) (CRE-luciferase) Reactive blue 2 Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 1.259↓ pK(b) (CRE-luciferase) PSB-0826 Hoffmann K et al (2009)
p2y12_human 5.43x43 194 TM5 C => A 14.493↑ pK(b) (CRE-luciferase) PSB-0739 Hoffmann K et al (2014)
p2y12_human 6.55x55 256 TM6 R => A 1.0 pK(b) (cAMP accumulation) Cangrelor Hoffmann K et al (2008)
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 2.512↓ pK(d) (CRE-luciferase) PSB-0739 Hoffmann K et al (2009)
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 => A 7.943↓ pK(b) (cAMP accumulation) Reactive blue 2 Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 1.122↑ pK(b) (cAMP accumulation) Ticagrelor Hoffmann K et al (2014)
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 => A 79.433↓ pIC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 3.981↓ pIC50 (CRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2009)
p2y12_human 3.29x29 101 TM3 S => A 1.259↓ pK(b) (cAMP accumulation) Cangrelor Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 6.429↓ IC50 (CRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 1.995↓ pK(b) (CRE-luciferase) Suramin Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => K 1.995↓ pK(b) (cAMP accumulation) Cangrelor Hoffmann K et al (2008)
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 3.981↓ pIC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 5.012↓ pK(b) (CRE-luciferase) PSB-0801 Hoffmann K et al (2009)
p2y12_human 5.43x43 194 TM5 C => A 6.761↓ pK(b) (CRE-luciferase) Ticagrelor Hoffmann K et al (2014)
p2y12_human 6.55x55 256 TM6 R => A 1.771↓ EC50 (SRE-luciferase) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 3.29x29 101 TM3 S => A 1.548↑ pK(b) (cAMP accumulation) Ticagrelor Hoffmann K et al (2014)
p2y12_human 6.55x55 256 TM6 R => D 501.187↓ pIC50 (cAMP accumulation) 2-methylthio-ADP Hoffmann K et al (2008)
p2y12_human 6.55x55 256 TM6 R => A 12.589↓ pK(b) (CRE-luciferase) MG 38-1 Hoffmann K et al (2009)
p2y12_human 5.43x43 194 TM5 C => A 3.636↑ pK(b) (CRE-luciferase) Reactive blue 2 Hoffmann K et al (2014)
p2y12_human 6.55x55 256 TM6 R => A 31.623↓ pK(b) (CRE-luciferase) Cibacron blue 3GA Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 5.012↓ pK(d) (CRE-luciferase) PSB-0739 Hoffmann K et al (2009)
p2y12_human 6.55x55 256 TM6 R => A 3.981↓ pK(b) (CRE-luciferase) Reactive blue 2 para Hoffmann K et al (2009)


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