YF-476 [Ligand Id: 887] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL324547 (Netazepida, Netazepide, Sograzepide, Yf476, YF-476) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
