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ChEMBL ligand: CHEMBL3236549 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human recombinant histamine H3 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis | B | 5.98 | pKi | 1043 | nM | Ki | J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018] |
GtoPdb | - | - | 6 | pKi | 1000 | nM | Ki | 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 | Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis | B | 7.9 | pKd | 12.59 | nM | Kd | J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018] |
ChEMBL | Agonist activity at human H4 receptor | B | 5 | pKi | >10000 | nM | Ki | J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018] |
GtoPdb | - | - | 7.9 | pKi | 12.5 | nM | Ki |
Pharmacol Rev (2015) 67: 601-55 [PMID:26084539]; J Med Chem (2014) 57: 2429-39 [PMID:24495018] |
ChEMBL | Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis | B | 7.9 | pKi | 12.5 | nM | Ki | J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018] |
ChEMBL | Displacement of [3H]histamine from human recombinant histamine H4 receptor | B | 7.92 | pKi | 12 | nM | Ki | Bioorg. Med. Chem. Lett. (2015) 25: 956-959 [PMID:25595684] |
ChEMBL | Displacement of [3H]histamine from human recombinant histamine H4 receptor | B | 7.92 | pKi | 12 | nM | Ki | J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395] |
H4 receptor/Histamine H4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5657] [GtoPdb: 265] [UniProtKB: Q91ZY2] | ||||||||
ChEMBL | Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis | B | 8.3 | pKd | 5.01 | nM | Kd | J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018] |
ChEMBL | Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis | B | 8.28 | pKi | 5.3 | nM | Ki | J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018] |
ChEMBL | Displacement of [3H]histamine from mouse recombinant histamine H4 receptor | B | 8.28 | pKi | 5.3 | 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 | Antagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis | B | 7.2 | pKd | 63.1 | nM | Kd | J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018] |
ChEMBL | Displacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis | B | 6.73 | pKi | 188 | nM | Ki | J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018] |
ChEMBL | Displacement of [3H]histamine from rat recombinant histamine H4 receptor | B | 6.73 | pKi | 188 | 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 | Binding affinity to guinea pig histamine H4 receptor | B | 6.51 | pKi | 306 | nM | Ki | J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018] |
ChEMBL | Displacement of [3H]histamine from guinea pig recombinant histamine H4 receptor | B | 6.51 | pKi | 306 | nM | Ki | J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395] |
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
GtoPdb | - | - | 6 | pKi | >1000 | nM | Ki | Pharmacol Rev (2015) 67: 601-55 [PMID:26084539] |
H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
GtoPdb | - | - | 6 | pKi | >1000 | nM | Ki | Pharmacol Rev (2015) 67: 601-55 [PMID:26084539] |
ChEMBL data shown on this page come from version 28:
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]