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, NVP-ZPL389-NX, Pf-03893787, PF-03893787, PF-3893787, ZPL-389, ZPL-3893787, ZPL-389-NX, ZPL389-NX)
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]
There should be some charts here, you may need to enable JavaScript!
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 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]