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 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]
