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

CHEMBL860282

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

Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-N-MC
Confidence 9 — Direct single protein target
Curated By Expert

Target

Histamine H4 receptor (CHEMBL3759)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
Venable JD, Cai H, Chai W, Dvorak CA, Grice CA, Jablonowski JA, Shah CR, Kwok AK, Ly KS, Pio B, Wei J, Desai PJ, Jiang W, Nguyen S, Ling P, Wilson SJ, Dunford PJ, Thurmond RL, Lovenberg TW, Karlsson L, Carruthers NI, Edwards JP.
J Med Chem (2005) 48 : 8289 -8298
PubMed 16366610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 7.47 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL199062 1 8.52
CHEMBL129198 JNJ-7777120 1 8.40
CHEMBL129436 1 8.30
CHEMBL120591 1 8.15
CHEMBL129488 1 8.15
CHEMBL128613 1 8.10
CHEMBL129540 1 8.10
CHEMBL338937 1 7.96
CHEMBL129444 1 7.85
CHEMBL436381 1 7.82
CHEMBL340740 1 7.82
CHEMBL129199 1 7.77
CHEMBL338051 1 7.72
CHEMBL333220 1 7.72
CHEMBL199231 1 7.68
CHEMBL128958 1 7.64
CHEMBL120854 1 7.64
CHEMBL364400 1 7.60
CHEMBL185951 1 7.58
CHEMBL268525 1 7.57
CHEMBL383384 1 7.52
CHEMBL129026 1 7.51
CHEMBL128505 1 7.50
CHEMBL187285 1 7.48
CHEMBL382276 1 7.46
CHEMBL129660 1 7.42
CHEMBL370135 1 7.40
CHEMBL128088 1 7.34
CHEMBL338972 1 7.31
CHEMBL128252 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL199062 Ki = 3.0 nM 8.52
CHEMBL129198 JNJ-7777120 Ki = 4.0 nM 8.40
CHEMBL129436 Ki = 5.0 nM 8.30
CHEMBL120591 Ki = 7.0 nM 8.15
CHEMBL129488 Ki = 7.0 nM 8.15
CHEMBL128613 Ki = 8.0 nM 8.10
CHEMBL129540 Ki = 8.0 nM 8.10
CHEMBL338937 Ki = 11.0 nM 7.96
CHEMBL129444 Ki = 14.0 nM 7.85
CHEMBL436381 Ki = 15.0 nM 7.82
CHEMBL340740 Ki = 15.0 nM 7.82
CHEMBL129199 Ki = 17.0 nM 7.77
CHEMBL338051 Ki = 19.0 nM 7.72
CHEMBL333220 Ki = 19.0 nM 7.72
CHEMBL199231 Ki = 21.0 nM 7.68
CHEMBL128958 Ki = 23.0 nM 7.64
CHEMBL120854 Ki = 23.0 nM 7.64
CHEMBL364400 Ki = 25.0 nM 7.60
CHEMBL185951 Ki = 26.0 nM 7.58
CHEMBL268525 Ki = 27.0 nM 7.57
CHEMBL383384 Ki = 30.0 nM 7.52
CHEMBL129026 Ki = 31.0 nM 7.51
CHEMBL128505 Ki = 32.0 nM 7.50
CHEMBL187285 Ki = 33.0 nM 7.48
CHEMBL382276 Ki = 35.0 nM 7.46
CHEMBL129660 Ki = 38.0 nM 7.42
CHEMBL370135 Ki = 40.0 nM 7.40
CHEMBL128088 Ki = 46.0 nM 7.34
CHEMBL338972 Ki = 49.0 nM 7.31
CHEMBL128252 Ki = 61.0 nM 7.21
CHEMBL200546 Ki = 90.0 nM 7.05
CHEMBL362495 Ki = 90.0 nM 7.05
CHEMBL120221 Ki = 136.0 nM 6.87
CHEMBL338001 Ki = 147.0 nM 6.83
CHEMBL2113162 Ki = 244.0 nM 6.61
CHEMBL197477 Ki = 412.0 nM 6.38
CHEMBL331773 Ki = 427.0 nM 6.37
CHEMBL121679 Ki = 528.0 nM 6.28
CHEMBL128637 Ki = 3000.0 nM 5.52