PD 128907 [Ligand Id: 952] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL97424 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Displacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cells after 60 mins by microbeta counting based assay | B | 4 | pKi | >100000 | nM | Ki | ACS Med Chem Lett (2020) 11: 1956-1964 [PMID:33062179] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D2L expressed in CHO K-1 cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2000) 43: 2871-2882 [PMID:10956195] |
| ChEMBL | Displacement of [3H]-(R)-(+)-7-OH-DPAT from human D2L receptor expressed in HEK293 cells after 90 mins by microbeta counting based assay | B | 5.12 | pKi | 7580 | nM | Ki | ACS Med Chem Lett (2020) 11: 1956-1964 [PMID:33062179] |
| GtoPdb | - | - | 6.4 | pKi | - | - | - |
Neuroreport (1995) 6: 329-332 [PMID:7756621]; J Pharmacol Exp Ther (1995) 275: 1355-66 [PMID:8531103] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Concentration inhibiting specific binding of [3H]haloperidol to Dopamine receptor D2 from rat striatal brain. | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1990) 33: 445-450 [PMID:1967318] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D3 expressed in CHO K-1 cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2000) 43: 2871-2882 [PMID:10956195] |
| ChEMBL | Displacement of [3H]-(R)-(+)-7-OH-DPAT from human D3 receptor expressed in HEK293 cells after 90 mins by microbeta counting based assay | B | 5.25 | pKi | 5620 | nM | Ki | ACS Med Chem Lett (2020) 11: 1956-1964 [PMID:33062179] |
| GtoPdb | - | - | 7.7 | pKi | 19.9 | nM | Ki |
Neuroreport (1995) 6: 329-332 [PMID:7756621]; J Pharmacol Exp Ther (1995) 275: 1355-66 [PMID:8531103] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Displacement of [3H]-DAMGO from human MOR expressed in HEK293 cells after 60 mins by microbeta counting based assay | B | 4.11 | pKi | 77900 | nM | Ki | ACS Med Chem Lett (2020) 11: 1956-1964 [PMID:33062179] |
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]
