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

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ChEMBL ligand: CHEMBL1915540 (Adriforant, PF-3893787, ZPL-3893787, PF-03893787, ZPL-389)
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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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 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]