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 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]
