quinelorane [Ligand Id: 954] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL155731 (Quinelorane) |
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1990) 33: 600-607 [PMID:2405158] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| GtoPdb | - | - | 5.7 | pKi | - | - | - |
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; J Pharmacol Exp Ther (1995) 275: 885-898 [PMID:7473180] |
| ChEMBL | Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | F | 7.35 | pEC50 | 45 | nM | EC50 | J Med Chem (2015) 58: 718-738 [PMID:25490054] |
| ChEMBL | Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay | F | 7.35 | pEC50 | 45 | nM | EC50 | Medchemcomm (2014) 5: 891-898 |
| ChEMBL | Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | F | 7.35 | pEC50 | 44.67 | nM | EC50 | J Med Chem (2015) 58: 718-738 [PMID:25490054] |
| ChEMBL | Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay | F | 7.35 | pEC50 | 44.67 | nM | EC50 | Medchemcomm (2014) 5: 891-898 |
| ChEMBL | Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation | F | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6691-6696 [PMID:17976986] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro binding affinity towards rat Dopamine receptor D2 by [3H]spiperone displacement. | B | 6.82 | pIC50 | 151 | nM | IC50 | J Med Chem (1990) 33: 600-607 [PMID:2405158] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| GtoPdb | - | - | 7.4 | pKi | - | - | - |
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; J Pharmacol Exp Ther (1995) 275: 885-898 [PMID:7473180] |
| ChEMBL | Inhibition constant against [3H]-spiperone binding to human Dopamine receptor D3 expressed in CHO cells | B | 9.03 | pKi | 0.93 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation | F | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6691-6696 [PMID:17976986] |
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]
