adriforant [Ligand Id: 8985] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1915540 (Adriforant, NVP-ZPL389-NX, Pf-03893787, PF-03893787, PF-3893787, ZPL-389, ZPL-3893787, ZPL-389-NX, ZPL389-NX) |
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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 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]
