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Assay Detail

CHEMBL4041923

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Binding
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL ↗
28
Total Activities
14
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 28 7.74 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4102970 — — 2 8.57
CHEMBL4065099 — — 2 8.52
CHEMBL4098585 — — 2 8.40
CHEMBL1223749 — — 2 8.28
CHEMBL1223750 — — 2 8.27
CHEMBL4063170 — — 2 7.96
CHEMBL4095224 — — 2 7.84
CHEMBL4082297 — — 2 7.72
CHEMBL1179089 — — 2 7.60
CHEMBL4100315 — — 2 7.57
CHEMBL1223748 — — 2 7.29
CHEMBL4084275 — — 2 7.21
CHEMBL4083336 — — 2 6.76
CHEMBL4072893 — — 2 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4102970 — Ki = 2.7 nM 8.57
CHEMBL4102970 — Ki = 2.7 nM 8.57
CHEMBL4065099 — Ki = 3.0 nM 8.52
CHEMBL4065099 — Ki = 3.0 nM 8.52
CHEMBL4098585 — Ki = 4.0 nM 8.40
CHEMBL4098585 — Ki = 4.0 nM 8.40
CHEMBL1223749 — Ki = 5.2 nM 8.28
CHEMBL1223749 — Ki = 5.2 nM 8.28
CHEMBL1223750 — Ki = 5.4 nM 8.27
CHEMBL1223750 — Ki = 5.4 nM 8.27
CHEMBL4063170 — Ki = 11.0 nM 7.96
CHEMBL4063170 — Ki = 11.0 nM 7.96
CHEMBL4095224 — Ki = 14.5 nM 7.84
CHEMBL4095224 — Ki = 14.5 nM 7.84
CHEMBL4082297 — Ki = 19.0 nM 7.72
CHEMBL4082297 — Ki = 19.0 nM 7.72
CHEMBL1179089 — Ki = 25.0 nM 7.60
CHEMBL1179089 — Ki = 25.0 nM 7.60
CHEMBL4100315 — Ki = 27.0 nM 7.57
CHEMBL4100315 — Ki = 27.0 nM 7.57
CHEMBL1223748 — Ki = 51.0 nM 7.29
CHEMBL1223748 — Ki = 51.0 nM 7.29
CHEMBL4084275 — Ki = 62.0 nM 7.21
CHEMBL4084275 — Ki = 62.0 nM 7.21
CHEMBL4083336 — Ki = 174.0 nM 6.76
CHEMBL4083336 — Ki = 174.0 nM 6.76
CHEMBL4072893 — Ki = 400.0 nM 6.40
CHEMBL4072893 — Ki = 400.0 nM 6.40