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Assay Detail

CHEMBL4371598

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Binding
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Tan L, Yan W, McCorvy JD, Cheng J.
J Med Chem (2018) 61 : 9841 -9878
PubMed 29939744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.00 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL563342 1 7.80
CHEMBL260549 1 7.60
CHEMBL551790 1 7.40
CHEMBL492677 1 7.20
CHEMBL2047474 1 6.00
CHEMBL1688969 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL563342 EC50 = 15.85 nM 7.80
CHEMBL260549 EC50 = 25.12 nM 7.60
CHEMBL551790 EC50 = 39.81 nM 7.40
CHEMBL492677 EC50 = 63.1 nM 7.20
CHEMBL2047474 EC50 = 1000.0 nM 6.00
CHEMBL1688969 EC50 = 1000.0 nM 6.00