YF-476 [Ligand Id: 887] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL324547 (Netazepide, Sograzepide, Yf476, YF-476) |
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1901] [GtoPdb: 76] [UniProtKB: P32238] | ||||||||
| ChEMBL | Binding affinity to human CCK1 receptor | B | 7.5 | pKi | 31.62 | nM | Ki | Bioorg Med Chem (2008) 16: 2974-2983 [PMID:18289857] |
| ChEMBL | Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line | B | 7.52 | pKi | 30.2 | nM | Ki | J Med Chem (2006) 49: 2253-2261 [PMID:16570921] |
| ChEMBL | Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells | B | 7.54 | pKi | 28.84 | nM | Ki | J Med Chem (2007) 50: 3101-3112 [PMID:17536796] |
| CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551] | ||||||||
| ChEMBL | Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas | B | 6.3 | pIC50 | 502 | nM | IC50 | J Med Chem (1997) 40: 331-341 [PMID:9022799] |
| GtoPdb | - | - | 6.9 | pIC50 | - | - | - | J Med Chem (1997) 40: 331-41 [PMID:9022799] |
| Cholecystokinin A receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3501] [UniProtKB: Q63931] | ||||||||
| ChEMBL | Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells | B | 6.4 | pKi | 398.11 | nM | Ki | J Med Chem (2008) 51: 565-573 [PMID:18201065] |
| CCK2 receptor/Cholecystokinin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239] | ||||||||
| GtoPdb | - | - | 9.6 | pKi | - | - | - | Regul Pept (2002) 103: 29-37 [PMID:11738246] |
| ChEMBL | Displacement of [125I]BH-CCK-8S from human recombinant CCK2 receptor expressed in NIH3T3 cells | B | 9.86 | pKi | 0.14 | nM | Ki | J Med Chem (2006) 49: 2253-2261 [PMID:16570921] |
| ChEMBL | Displacement of [3H]BH-CCK-8S from human recombinant CCK2 receptor expressed in NIH3T3 cells | B | 9.86 | pKi | 0.14 | nM | Ki | J Med Chem (2007) 50: 3101-3112 [PMID:17536796] |
| ChEMBL | Binding affinity at human CCK2 receptor | B | 10.1 | pKi | 0.08 | nM | Ki | Bioorg Med Chem (2008) 16: 2974-2983 [PMID:18289857] |
| GtoPdb | - | - | 9.7 | pIC50 | - | - | - |
Aliment Pharmacol Ther (2012) 36: 181-9 [PMID:22607579]; Aliment Pharmacol Ther (1997) 11: 113-20 [PMID:9042983] |
| CCK2 receptor/Cholecystokinin B receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3508] [GtoPdb: 77] [UniProtKB: P30553] | ||||||||
| ChEMBL | Affinity for CCK2 receptor assessed by inhibition of pentagastrin-stimulated acid secretion in perfused rat stomach | F | 10.1 | pKd | 0.08 | nM | Kd | J Med Chem (2006) 49: 2253-2261 [PMID:16570921] |
| ChEMBL | Antagonist activity at CCK2 receptor in perfused rat stomach assessed as inhibition of pentagastrin-stimulated gastric acid secretion | F | 10.1 | pKd | 0.08 | nM | Kd | J Med Chem (2007) 50: 3101-3112 [PMID:17536796] |
| ChEMBL | Inhibitory concentration against radioligand [125I]CCK-8 binding to gastrin/Cholecystokinin type B receptor from rat brain | B | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (1997) 40: 331-341 [PMID:9022799] |
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]
