lorglumide [Ligand Id: 891] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL24938 (CR-1409, 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 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]
