nafadotride [Ligand Id: 44] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL286252 (nafadotride)
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
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  • D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor in Rat [GtoPdb: 215] [UniProtKB: P61169]
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  • D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells B 9.09 pKi 0.81 nM Ki J Med Chem (2003) 46: 4377-4392 [PMID:14521403]
GtoPdb - - 9.52 pKi 0.3 nM Ki J Pharmacol Exp Ther (1995) 275: 1239-46 [PMID:8531087]
ChEMBL Binding affinity against Dopamine receptor D3 B 9.96 pKi 0.11 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 7.3 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]
D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb - - 8.5 pKi - - - J Pharmacol Exp Ther (1995) 275: 1239-46 [PMID:8531087]
D2 receptor in Rat [GtoPdb: 215] [UniProtKB: P61169]
GtoPdb - - 8.8 pKi - - - Mol Pharmacol (2000) 57: 144-52 [PMID:10617689]
D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729]
GtoPdb - - 6.4 pKi - - - Mol Pharmacol (2000) 57: 144-52 [PMID:10617689]

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]