chlorpheniramine [Ligand Id: 6976] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL505 (Antagonate, Chlorphenamine, Chlorpheniramine, Chlor-Trimeton, Isoclor, Kloromin, Phenetron, Teldrin)
  • Chloroquine resistance transporter in Plasmodium falciparum [ChEMBL: CHEMBL1795182] [UniProtKB: Q9N623]
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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]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
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  • Lethal(3)malignant brain tumor-like protein 1 in Human [ChEMBL: CHEMBL1287622] [UniProtKB: Q9Y468]
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  • L3MBTL histone methyl-lysine binding protein 3/Lethal(3)malignant brain tumor-like protein 3 in Human [ChEMBL: CHEMBL1287623] [GtoPdb: 2830] [UniProtKB: Q96JM7]
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  • Lethal(3)malignant brain tumor-like protein 4 in Human [ChEMBL: CHEMBL1287624] [UniProtKB: Q8NA19]
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  • PAF receptor/Platelet activating factor receptor in Human [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Rat [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Rat [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Chloroquine resistance transporter in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795182] [UniProtKB: Q9N623]
ChEMBL Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes plasma membrane assessed as reduction of [3H]-chloroquine transportation after 1 to 2 hrs B 4.27 pIC50 54000 nM IC50 ACS Med Chem Lett (2014) 5: 576-581 [PMID:24900883]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 4.68 pIC50 20892.96 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibitory concentration against potassium channel HERG B 4.68 pIC50 20892.96 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 4.68 pIC50 20892.96 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG B 4.68 pIC50 20892.96 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibitory concentration against IKr potassium channel B 5.96 pIC50 1100 nM IC50 Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 8.15 pKi 7 nM Ki J Med Chem (2011) 54: 2183-95 [PMID:21381763]
ChEMBL Binding affinity to histamine H1 receptor B 8.15 pKi 7 nM Ki J Med Chem (2011) 54: 2183-2195 [PMID:21381763]
ChEMBL Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin) B 8.35 pKi 4.47 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin) B 9.04 pKi 0.92 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells B 7.18 pIC50 66 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand B 8.26 pKi 5.5 nM Ki J Med Chem (1991) 34: 457-461 [PMID:1671420]
ChEMBL Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes B 8.26 pKi 5.5 nM Ki Bioorg Med Chem Lett (1998) 8: 3469-3474 [PMID:9934454]
ChEMBL Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes B 8.7 pKi 2 nM Ki Bioorg Med Chem Lett (2003) 13: 1959-1961 [PMID:12781173]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex B 8.06 pIC50 8.8 nM IC50 J Med Chem (1991) 34: 1314-1328 [PMID:1673158]
Lethal(3)malignant brain tumor-like protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287622] [UniProtKB: Q9Y468]
ChEMBL Inhibition of L3MBTL1 by alpha-screening B 4.39 pIC50 41000 nM IC50 J Med Chem (2010) 53: 7625-7631 [PMID:20931980]
L3MBTL histone methyl-lysine binding protein 3/Lethal(3)malignant brain tumor-like protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287623] [GtoPdb: 2830] [UniProtKB: Q96JM7]
ChEMBL Inhibition of L3MBTL3 by alpha-screening B 4.38 pIC50 42000 nM IC50 J Med Chem (2010) 53: 7625-7631 [PMID:20931980]
Lethal(3)malignant brain tumor-like protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287624] [UniProtKB: Q8NA19]
ChEMBL Inhibition of L3MBTL4 by alpha-screening B 4 pIC50 >100000 nM IC50 J Med Chem (2010) 53: 7625-7631 [PMID:20931980]
MBT domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287625] [UniProtKB: Q05BQ5]
ChEMBL Inhibition of MBTD1 by alpha-screening B 4.47 pIC50 34000 nM IC50 J Med Chem (2010) 53: 7625-7631 [PMID:20931980]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes by SYBR green assay F 4.21 pIC50 61200 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
ChEMBL Antimalarial activity after 72 hrs against chloroquine-resistant Plasmodium falciparum Dd2 infected human erythrocytes by SYBR green assay F 5.41 pIC50 3900 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
PAF receptor/Platelet activating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
ChEMBL Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when challenged with 25 nM PAF. F 4.3 pIC50 >50000 nM IC50 J Med Chem (1991) 34: 457-461 [PMID:1671420]
Organic cation transporter 1/Solute carrier family 22 member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells F 4.85 pIC50 14000 nM IC50 Pharm Res (2001) 18: 1528-1534 [PMID:11758759]
Organic cation transporter 2/Solute carrier family 22 member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells F 4.59 pIC50 26000 nM IC50 Pharm Res (2001) 18: 1528-1534 [PMID:11758759]

ChEMBL data shown on this page come from version 32:

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]