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ChEMBL ligand: CHEMBL3785736 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]