lorglumide [Ligand Id: 891] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL24938 (CR-1409, Lorglumida, Lorglumide) |
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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 | 6.89 | pKi | 129 | nM | Ki | J Med Chem (1996) 39: 860-872 [PMID:8632410] |
| ChEMBL | Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (1992) 35: 28-38 [PMID:1732532] |
| ChEMBL | Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 1251-1256 |
| ChEMBL | Inhibition of binding of [125I]- CCK-33 to rat pancreas | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (1990) 33: 591-595 [PMID:2299627] |
| GtoPdb | - | - | 8.2 | pIC50 | 6.31 | nM | IC50 |
Proc Natl Acad Sci USA (1990) 87: 6728-32 [PMID:1975695]; Pancreas (1987) 2: 85-90 [PMID:2437574] |
| Cholecystokinin A receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3501] [UniProtKB: Q63931] | ||||||||
| ChEMBL | Inhibition of binding of [125I]- CCK-33 to guinea pig cortex | B | 5.66 | pIC50 | 2200 | nM | IC50 | J Med Chem (1990) 33: 591-595 [PMID:2299627] |
| CCK2 receptor/Cholecystokinin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239] | ||||||||
| ChEMBL | Concentration required to inhibit by 50% the specific binding of [3H]pentagastrin to cholecystokinin type B receptor in rabbit gastric gland | B | 4.6 | pIC50 | 25000 | nM | IC50 | J Med Chem (1992) 35: 28-38 [PMID:1732532] |
| GtoPdb | - | - | 5.5 | pIC50 | - | - | - | Neuropeptides (1996) 30: 359-63 [PMID:8914862] |
| ChEMBL | Inhibition of binding of [125I]gastrin to Cholecystokinin type B receptor from guinea pig gastric glands | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1990) 33: 591-595 [PMID:2299627] |
| ChEMBL | Displacement of [125I]CCK-OP radioligand from Cholecystokinin type B receptor of guinea pig cortical membranes | B | 6 | pIC50 | >>1000 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 1251-1256 |
| CCK2 receptor/Cholecystokinin B receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3508] [GtoPdb: 77] [UniProtKB: P30553] | ||||||||
| ChEMBL | Inhibition of the specific binding of [125I](BH)-CCK-8 to Cholecystokinin type B receptor in rat brain cortex | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (1992) 35: 28-38 [PMID:1732532] |
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]
