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 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]