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 35:
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]
