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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 |
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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 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]