AM-0902 [Ligand Id: 10276] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3785736
  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
ChEMBL Antagonist activity at human TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced 45Ca2+ uptake preincubated for 1 min followed by AITC addition measured after 12 mins B 6.88 pIC50 131 nM IC50 J Med Chem (2016) 59: 2794-2809 [PMID:26942860]
ChEMBL Antagonist activity at human TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced Ca2+ influx preincubated for 2 mins followed by AITC addition measured for 2 mins by Fluo-4 dye based FLIPR assay B 7.7 pIC50 20 nM IC50 J Med Chem (2016) 59: 2794-2809 [PMID:26942860]
GtoPdb Antagonism of activator-induced calcium flux measuring 45Ca2+. - 7.7 pIC50 20 nM IC50 J Med Chem (2016) 59: 2794-809 [PMID:26942860]
ChEMBL Agonist activity at human TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells by 45Ca2+ uptake assay B 4.4 pEC50 >40000 nM EC50 J Med Chem (2016) 59: 2794-2809 [PMID:26942860]
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86]
ChEMBL Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced 45Ca2+ uptake preincubated for 1 min followed by AITC addition measured after 12 mins B 7.15 pIC50 71 nM IC50 J Med Chem (2016) 59: 2794-2809 [PMID:26942860]
GtoPdb Antagonism of activator-induced calcium flux measuring 45Ca2+. - 7.62 pIC50 24 nM IC50 J Med Chem (2016) 59: 2794-809 [PMID:26942860]
ChEMBL Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced Ca2+ influx preincubated for 2 mins followed by AITC addition measured for 2 mins by Fluo-4 dye based FLIPR assay B 7.7 pIC50 20 nM IC50 J Med Chem (2016) 59: 2794-2809 [PMID:26942860]
ChEMBL Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of methylglyoxal-induced 45Ca2+ uptake preincubated for 10 mins followed by methylglyoxal addition measured after 3 mins by TopCount microplate scintillator counting method B 7.72 pIC50 19 nM IC50 J Med Chem (2016) 59: 2794-2809 [PMID:26942860]
ChEMBL Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of hypo osmolarity buffer-induced 45Ca2+ uptake preincubated for 10 mins followed by hypo osmolarity buffer addition measured after 3 mins by TopCount microplate scintillator counting method B 8 pIC50 10 nM IC50 J Med Chem (2016) 59: 2794-2809 [PMID:26942860]
ChEMBL Agonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells by 45Ca2+ uptake assay B 4.4 pEC50 >40000 nM EC50 J Med Chem (2016) 59: 2794-2809 [PMID:26942860]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]