chlorprothixene [Ligand Id: 11976] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL908 (Chlorprothixene, N-714, N-714RO 4-0403, NSC-18720, RO 4-0403, RO-4-0403, RO-40403, Taractan, Truxal)
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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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 dopamine D1 receptor expressed in HEK cells B 7.74 pKi 18 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells B 8.53 pKi 2.96 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
GtoPdb - - 8.53 pKi 2.96 nM Ki Bioorg Med Chem Lett (2009) 19: 538-42 [PMID:19091563]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
GtoPdb - - 8.34 pKi 4.56 nM Ki Bioorg Med Chem Lett (2009) 19: 538-42 [PMID:19091563]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells B 8.34 pKi 4.56 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells B 8.05 pKi 9 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells B 8.43 pKi 3.75 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
GtoPdb - - 8.43 pKi 3.75 nM Ki Bioorg Med Chem Lett (2009) 19: 538-42 [PMID:19091563]
ChEMBL Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay F 6.06 pIC50 870.96 nM IC50 J Med Chem (2012) 55: 7054-7060 [PMID:22793499]
ChEMBL Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay F 9 pIC50 1 nM IC50 J Med Chem (2012) 55: 7054-7060 [PMID:22793499]
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting B 8.97 pIC50 1.07 nM IC50 J Med Chem (2012) 55: 7054-7060 [PMID:22793499]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO/HEK293 cells B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
ChEMBL Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay B 5.29 pIC50 5100 nM IC50 Antimicrob Agents Chemother (2009) 53: 1516-1527 [PMID:19188399]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 6 receptor B 8.52 pKi 3 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Binding affinity towards rat 5-hydroxytryptamine 7 receptor B 8.25 pKi 5.6 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.11 pIC50 77800 nM IC50 J Med Chem (2008) 51: 5932-5942 [PMID:18788725]

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]