adriforant [Ligand Id: 8985] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1915540 (Adriforant, PF-3893787, ZPL-3893787, PF-03893787, ZPL-389)
  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 1 pki data point
1 CHEMBL1915540_lig_chart_1 HERG Human
There should be some charts here, you may need to enable JavaScript!
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
2 CHEMBL1915540_lig_chart_2 Histamine H3 receptor Human
There should be some charts here, you may need to enable JavaScript!
3 CHEMBL1915540_lig_chart_3 Histamine H4 receptor HumanMouseRatGuinea pig
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]astemizole from human ERG channel B 5.46 pKi 3467.37 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 2663-2670 [PMID:23558237]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Displacement of [3H]histamine from human histamine H3 receptor expressed in HEK cells B 6.73 pKi 186.21 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 2663-2670 [PMID:23558237]
GtoPdb - - 6.73 pKi - - - Pharmacol. Rev. (2015) 67: 601-55 [PMID:26084539]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis B 7.6 pKd 25.12 nM Kd Bioorg. Med. Chem. Lett. (2013) 23: 2663-2670 [PMID:23558237]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells B 7.99 pKi 10.23 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 2663-2670 [PMID:23558237]
ChEMBL Displacement of [3H]-histamine from human H4R expressed in HEK293T cells B 8.21 pKi 6.17 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 6596-6602 [PMID:21920751]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells B 8.21 pKi 6.17 nM Ki J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395]
GtoPdb - - 8.31 pKi - - - Pharmacol. Rev. (2015) 67: 601-55 [PMID:26084539]
ChEMBL Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cells B 8.62 pKi 2.4 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 6596-6602 [PMID:21920751]
ChEMBL Binding affinity to human histamine H4 receptor B 8.62 pKi 2.4 nM Ki J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395]
ChEMBL Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay F 8.81 pKi 1.56 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 6596-6602 [PMID:21920751]
ChEMBL Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding F 7.27 pIC50 53.7 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 2663-2670 [PMID:23558237]
ChEMBL Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay F 7.52 pIC50 <30 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6596-6602 [PMID:21920751]
ChEMBL Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation F 8.31 pIC50 4.9 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6596-6602 [PMID:21920751]
ChEMBL Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation F 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6596-6602 [PMID:21920751]
ChEMBL Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay F 9.19 pIC50 0.65 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6596-6602 [PMID:21920751]
H4 receptor/Histamine H4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5657] [GtoPdb: 265] [UniProtKB: Q91ZY2]
ChEMBL Binding affinity to mouse histamine H4 receptor B 7.26 pKi 54.95 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 2663-2670 [PMID:23558237]
ChEMBL Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cells B 7.68 pKi 20.89 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 6596-6602 [PMID:21920751]
ChEMBL Displacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cells B 7.68 pKi 20.89 nM Ki J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395]
H4 receptor/Histamine H4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4468] [GtoPdb: 265] [UniProtKB: Q91ZY1]
ChEMBL Binding affinity to rat histamine H4 receptor B 7.26 pKi 54.95 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 2663-2670 [PMID:23558237]
ChEMBL Displacement of [3H]-histamine from rat H4R expressed in HEK293T cells B 7.91 pKi 12.3 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 6596-6602 [PMID:21920751]
ChEMBL Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cells B 7.91 pKi 12.3 nM Ki J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395]
Histamine H4 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255160] [UniProtKB: Q91ZY3]
ChEMBL Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells B 6.91 pKi 123.03 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 6596-6602 [PMID:21920751]
ChEMBL Displacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cells B 6.91 pKi 123.03 nM Ki J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]