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Assay Detail

CHEMBL4041924

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

Binding
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
22
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of nanomolar ligands with novel scaffolds for the histamine H4 receptor by virtual screening.
Levoin N, Labeeuw O, Billot X, Calmels T, Danvy D, Krief S, Berrebi-Bertrand I, Lecomte JM, Schwartz JC, Capet M.
Eur J Med Chem (2017) 125 : 565 -572
PubMed 27718472 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 5.78 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20338 2 6.93
CHEMBL1223683 2 6.90
CHEMBL4102243 2 6.67
CHEMBL91576 2 6.62
CHEMBL4092578 2 5.96
CHEMBL4061504 2 5.52
CHEMBL4099779 2 5.42
CHEMBL4085023 2 5.38
CHEMBL4096444 2 4.89
CHEMBL4062122 2 4.79
CHEMBL4084820 2 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20338 Ki = 118.0 nM 6.93
CHEMBL20338 Ki = 118.0 nM 6.93
CHEMBL1223683 Ki = 125.0 nM 6.90
CHEMBL1223683 Ki = 125.0 nM 6.90
CHEMBL4102243 Ki = 214.0 nM 6.67
CHEMBL4102243 Ki = 214.0 nM 6.67
CHEMBL91576 Ki = 240.0 nM 6.62
CHEMBL91576 Ki = 240.0 nM 6.62
CHEMBL4092578 Ki = 1090.0 nM 5.96
CHEMBL4092578 Ki = 1090.0 nM 5.96
CHEMBL4061504 Ki = 3018.0 nM 5.52
CHEMBL4061504 Ki = 3018.0 nM 5.52
CHEMBL4099779 Ki = 3800.0 nM 5.42
CHEMBL4099779 Ki = 3800.0 nM 5.42
CHEMBL4085023 Ki = 4200.0 nM 5.38
CHEMBL4085023 Ki = 4200.0 nM 5.38
CHEMBL4096444 Ki = 13000.0 nM 4.89
CHEMBL4096444 Ki = 13000.0 nM 4.89
CHEMBL4062122 Ki = 16400.0 nM 4.79
CHEMBL4062122 Ki = 16400.0 nM 4.79
CHEMBL4084820 Ki = 30000.0 nM 4.52
CHEMBL4084820 Ki = 30000.0 nM 4.52