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) |
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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 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]
