AMG 9810 [Ligand Id: 6347] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL195789 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| ChEMBL | Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells | F | 5.49 | pIC50 | 3200 | nM | IC50 | J Med Chem (2005) 48: 71-90 [PMID:15634002] |
| ChEMBL | Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells | F | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2005) 48: 71-90 [PMID:15634002] |
| ChEMBL | Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells | F | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2005) 48: 71-90 [PMID:15634002] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay | F | 7.03 | pIC50 | 93 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay | F | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells | F | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2005) 48: 71-90 [PMID:15634002] |
| GtoPdb | - | - | 7.8 | pIC50 | - | - | - | J Pharmacol Exp Ther (2005) 313: 474-84 [PMID:15615864] |
| ChEMBL | Agonist activity at TRPV1 expressed in CHO cells | F | 5.4 | pEC50 | >4000 | nM | EC50 | J Med Chem (2007) 50: 3497-3514 [PMID:17585749] |
| TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] | ||||||||
| ChEMBL | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx | F | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (2007) 50: 3497-3514 [PMID:17585749] |
| ChEMBL | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay | F | 6.53 | pIC50 | 294 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay | F | 7.07 | pIC50 | 86 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx | F | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (2007) 50: 3497-3514 [PMID:17585749] |
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]
