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Assay Detail

CHEMBL3136604

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

Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Mapping histamine H4receptorligand binding modes
Schultes S, Nijmeijer S, Engelhardt H, Kooistra AJ, Vischer HF, de Esch IJP, Haaksma EEJ, Leurs R, de Graaf C
Medchemcomm (2013) 4 : 193 -204
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.59 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL493720 1 8.70
CHEMBL3133130 1 8.30
CHEMBL492884 1 8.30
CHEMBL3133131 1 8.10
CHEMBL494648 1 7.80
CHEMBL129198 JNJ-7777120 1 7.70
CHEMBL340740 1 7.60
CHEMBL129199 1 7.10
CHEMBL2047270 1 7.00
CHEMBL128637 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL493720 Ki = 1.995 nM 8.70
CHEMBL3133130 Ki = 5.012 nM 8.30
CHEMBL492884 Ki = 5.012 nM 8.30
CHEMBL3133131 Ki = 7.943 nM 8.10
CHEMBL494648 Ki = 15.85 nM 7.80
CHEMBL129198 JNJ-7777120 Ki = 19.95 nM 7.70
CHEMBL340740 Ki = 25.12 nM 7.60
CHEMBL129199 Ki = 79.43 nM 7.10
CHEMBL2047270 Ki = 100.0 nM 7.00
CHEMBL128637 Ki = 5011.87 nM 5.30