tifluadom [Ligand Id: 1667] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL169703 (KC-5103, Tifluadom) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551] | ||||||||
| ChEMBL | Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas. | B | 7.33 | pKi | 47 | nM | Ki | J Med Chem (1996) 39: 860-872 [PMID:8632410] |
| ChEMBL | Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (1990) 33: 450-455 [PMID:2153212] |
| CCK2 receptor/Cholecystokinin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239] | ||||||||
| ChEMBL | Binding affinity against Cholecystokinin type B receptor using [3H](MeNLE28,31)-CCK-8 as radioligand in guinea pig cerebral cortex. | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (1996) 39: 860-872 [PMID:8632410] |
| ChEMBL | Inhibition of binding of [125I]CCK-8 to Cholecystokinin type B receptor in guinea pig brain tissues | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1990) 33: 450-455 [PMID:2153212] |
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor delta 1 using [3H]DADLE as radioligand in guinea pig brain | B | 6.82 | pKi | 153 | nM | Ki | J Med Chem (1996) 39: 860-872 [PMID:8632410] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| GtoPdb | - | - | 8.8 | pKi | - | - | - | J Pharmacol Exp Ther (1997) 282: 676-84 [PMID:9262330] |
| ChEMBL | Binding affinity to kappa opioid receptor | B | 9.77 | pKi | 0.17 | nM | Ki | Bioorg Med Chem (2010) 18: 4446-4452 [PMID:20478711] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor kappa 1 of guinea pig using [3H]U-65693 as radioligand | B | 9.11 | pKi | 0.78 | nM | Ki | J Med Chem (1996) 39: 860-872 [PMID:8632410] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor mu 1 using [3H]-DAMGO as radioligand in guinea pig brain | B | 8.71 | pKi | 1.93 | nM | Ki | J Med Chem (1996) 39: 860-872 [PMID:8632410] |
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]
