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Assay Detail

CHEMBL1037060

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

Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.
Semple G, Tran TA, Kramer B, Hsu D, Han S, Choi J, Vallar P, Casper MD, Zou N, Hauser EK, Thomsen W, Whelan K, Sengupta D, Morgan M, Sekiguchi Y, Kanuma K, Chaki S, Grottick AJ.
Bioorg Med Chem Lett (2009) 19 : 6166 -6171
PubMed 19773162 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.40 6.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182150 1 6.98
CHEMBL568400 1 6.89
CHEMBL583014 1 6.70
CHEMBL577904 1 6.68
CHEMBL566075 1 6.51
CHEMBL565551 1 6.33
CHEMBL567993 1 6.24
CHEMBL567791 1 6.14
CHEMBL577912 1 5.80
CHEMBL578170 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182150 IC50 = 104.0 nM 6.98
CHEMBL568400 IC50 = 130.0 nM 6.89
CHEMBL583014 IC50 = 200.0 nM 6.70
CHEMBL577904 IC50 = 210.0 nM 6.68
CHEMBL566075 IC50 = 310.0 nM 6.51
CHEMBL565551 IC50 = 470.0 nM 6.33
CHEMBL567993 IC50 = 580.0 nM 6.24
CHEMBL567791 IC50 = 730.0 nM 6.14
CHEMBL577912 IC50 = 1590.0 nM 5.80
CHEMBL578170 IC50 = 1770.0 nM 5.75