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Assay Detail

CHEMBL700770

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

Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptor
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

The first potent and selective non-imidazole human histamine H4 receptor antagonists.
Jablonowski JA, Grice CA, Chai W, Dvorak CA, Venable JD, Kwok AK, Ly KS, Wei J, Baker SM, Desai PJ, Jiang W, Wilson SJ, Thurmond RL, Karlsson L, Edwards JP, Lovenberg TW, Carruthers NI.
J Med Chem (2003) 46 : 3957 -3960
PubMed 12954048 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 7.32 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129198 JNJ-7777120 1 8.40
CHEMBL129436 1 8.30
CHEMBL129488 1 8.15
CHEMBL129540 1 8.10
CHEMBL128613 1 8.10
CHEMBL338937 1 7.96
CHEMBL129444 1 7.85
CHEMBL340740 1 7.82
CHEMBL436381 1 7.82
CHEMBL129199 1 7.77
CHEMBL338051 1 7.72
CHEMBL128958 1 7.64
CHEMBL129026 1 7.51
CHEMBL128505 1 7.50
CHEMBL129660 1 7.42
CHEMBL128088 1 7.34
CHEMBL128252 1 7.21
CHEMBL338001 1 6.83
CHEMBL341087 1 6.70
CHEMBL128134 1 6.58
CHEMBL128637 1 5.52
CHEMBL128470 1 5.16
CHEMBL339826 1 5.00
CHEMBL128506 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129198 JNJ-7777120 Ki = 4.0 nM 8.40
CHEMBL129436 Ki = 5.0 nM 8.30
CHEMBL129488 Ki = 7.0 nM 8.15
CHEMBL129540 Ki = 8.0 nM 8.10
CHEMBL128613 Ki = 8.0 nM 8.10
CHEMBL338937 Ki = 11.0 nM 7.96
CHEMBL129444 Ki = 14.0 nM 7.85
CHEMBL340740 Ki = 15.0 nM 7.82
CHEMBL436381 Ki = 15.0 nM 7.82
CHEMBL129199 Ki = 17.0 nM 7.77
CHEMBL338051 Ki = 19.0 nM 7.72
CHEMBL128958 Ki = 23.0 nM 7.64
CHEMBL129026 Ki = 31.0 nM 7.51
CHEMBL128505 Ki = 32.0 nM 7.50
CHEMBL129660 Ki = 38.0 nM 7.42
CHEMBL128088 Ki = 46.0 nM 7.34
CHEMBL128252 Ki = 61.0 nM 7.21
CHEMBL338001 Ki = 147.0 nM 6.83
CHEMBL341087 Ki = 202.0 nM 6.70
CHEMBL128134 Ki = 260.0 nM 6.58
CHEMBL128637 Ki = 3000.0 nM 5.52
CHEMBL128470 Ki = 7000.0 nM 5.16
CHEMBL339826 Ki = 10000.0 nM 5.00
CHEMBL128506 Ki > 10000.0 nM -