Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1027436

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL ↗
77
Total Activities
77
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H4 receptor (CHEMBL4468) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.
Altenbach RJ, Adair RM, Bettencourt BM, Black LA, Fix-Stenzel SR, Gopalakrishnan SM, Hsieh GC, Liu H, Marsh KC, McPherson MJ, Milicic I, Miller TR, Vortherms TA, Warrior U, Wetter JM, Wishart N, Witte DG, Honore P, Esbenshade TA, Hancock AA, Brioni JD, Cowart MD.
J Med Chem (2008) 51 : 6571 -6580
PubMed 18811133 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 76 6.19 7.81
pKb 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492242 — — 1 7.81
CHEMBL492287 — — 1 7.50
CHEMBL493720 — — 1 7.43
CHEMBL492884 — — 1 7.40
CHEMBL492274 — — 1 7.37
CHEMBL493478 — — 1 7.37
CHEMBL493719 — — 1 7.36
CHEMBL444782 — — 1 7.33
CHEMBL492885 — — 1 7.25
CHEMBL494678 — — 1 7.23
CHEMBL492900 — — 1 7.23
CHEMBL446896 — — 1 7.18
CHEMBL492631 — — 1 7.17
CHEMBL505061 — — 1 7.16
CHEMBL507063 — — 1 7.03
CHEMBL494724 — — 1 6.99
CHEMBL494576 — — 1 6.99
CHEMBL501882 — — 1 6.94
CHEMBL494648 — — 1 6.94
CHEMBL502104 — — 1 6.93
CHEMBL522841 — — 1 6.76
CHEMBL494723 — — 1 6.75
CHEMBL522679 — — 1 6.71
CHEMBL492227 — — 1 6.68
CHEMBL493229 — — 1 6.66
CHEMBL473662 — — 1 6.66
CHEMBL492241 — — 1 6.64
CHEMBL495082 — — 1 6.63
CHEMBL522019 — — 1 6.63
CHEMBL506187 — — 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492242 — EC50 = 15.49 nM 7.81
CHEMBL492287 — EC50 = 31.62 nM 7.50
CHEMBL493720 — EC50 = 37.15 nM 7.43
CHEMBL492884 — EC50 = 39.81 nM 7.40
CHEMBL492274 — EC50 = 42.66 nM 7.37
CHEMBL493478 — EC50 = 42.66 nM 7.37
CHEMBL493719 — EC50 = 43.65 nM 7.36
CHEMBL444782 — EC50 = 46.77 nM 7.33
CHEMBL492885 — EC50 = 56.23 nM 7.25
CHEMBL494678 — EC50 = 58.88 nM 7.23
CHEMBL492900 — EC50 = 58.88 nM 7.23
CHEMBL446896 — EC50 = 66.07 nM 7.18
CHEMBL492631 — EC50 = 67.61 nM 7.17
CHEMBL505061 — EC50 = 69.18 nM 7.16
CHEMBL507063 — EC50 = 93.33 nM 7.03
CHEMBL494724 — EC50 = 102.33 nM 6.99
CHEMBL494576 — EC50 = 102.33 nM 6.99
CHEMBL501882 — EC50 = 114.82 nM 6.94
CHEMBL494648 — EC50 = 114.82 nM 6.94
CHEMBL502104 — EC50 = 117.49 nM 6.93
CHEMBL522841 — EC50 = 173.78 nM 6.76
CHEMBL494723 — EC50 = 177.83 nM 6.75
CHEMBL522679 — EC50 = 194.98 nM 6.71
CHEMBL492227 — EC50 = 208.93 nM 6.68
CHEMBL473662 — EC50 = 218.78 nM 6.66
CHEMBL493229 — EC50 = 218.78 nM 6.66
CHEMBL492241 — EC50 = 229.09 nM 6.64
CHEMBL495082 — EC50 = 234.42 nM 6.63
CHEMBL522019 — EC50 = 234.42 nM 6.63
CHEMBL506187 — EC50 = 245.47 nM 6.61
CHEMBL494890 — EC50 = 245.47 nM 6.61
CHEMBL494679 — EC50 = 251.19 nM 6.60
CHEMBL492288 — EC50 = 275.42 nM 6.56
CHEMBL495341 — EC50 = 302.0 nM 6.52
CHEMBL522661 — EC50 = 316.23 nM 6.50
CHEMBL444484 — EC50 = 338.84 nM 6.47
CHEMBL492662 — EC50 = 354.81 nM 6.45
CHEMBL493479 — EC50 = 363.08 nM 6.44
CHEMBL494667 — EC50 = 389.05 nM 6.41
CHEMBL495112 — EC50 = 489.78 nM 6.31
CHEMBL492677 — EC50 = 489.78 nM 6.31
CHEMBL493477 — EC50 = 630.96 nM 6.20
CHEMBL442865 — EC50 = 891.25 nM 6.05
CHEMBL495342 — EC50 = 933.25 nM 6.03
CHEMBL493099 — EC50 = 1122.02 nM 5.95
CHEMBL495083 — EC50 = 1202.26 nM 5.92
CHEMBL492869 — EC50 = 1348.96 nM 5.87
CHEMBL494909 — EC50 = 1479.11 nM 5.83
CHEMBL499631 — EC50 = 1778.28 nM 5.75
CHEMBL445091 — EC50 = 1819.7 nM 5.74