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Assay Detail

CHEMBL1763646

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Functional
Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mas-related G-protein coupled receptor member X1 (CHEMBL5850)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of 2,4-diaminopyrimidine derivatives as novel SNSR4 antagonists.
Bayrakdarian M, Butterworth J, Hu YJ, Santhakumar V, Tomaszewski MJ.
Bioorg Med Chem Lett (2011) 21 : 2102 -2105
PubMed 21333534 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.82 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1762707 1 7.85
CHEMBL1762698 1 7.70
CHEMBL1762699 1 7.66
CHEMBL1762700 1 7.62
CHEMBL1762701 1 7.40
CHEMBL1760000 1 7.11
CHEMBL1762702 1 7.06
CHEMBL1762705 1 6.97
CHEMBL1762703 1 6.61
CHEMBL1762704 1 6.53
CHEMBL1762696 1 6.52
CHEMBL1762706 1 6.48
CHEMBL1762693 1 6.28
CHEMBL1762695 1 6.19
CHEMBL1762697 1 6.12
CHEMBL1762694 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1762707 IC50 = 14.0 nM 7.85
CHEMBL1762698 IC50 = 20.0 nM 7.70
CHEMBL1762699 IC50 = 22.0 nM 7.66
CHEMBL1762700 IC50 = 24.0 nM 7.62
CHEMBL1762701 IC50 = 40.0 nM 7.40
CHEMBL1760000 IC50 = 77.0 nM 7.11
CHEMBL1762702 IC50 = 88.0 nM 7.06
CHEMBL1762705 IC50 = 108.0 nM 6.97
CHEMBL1762703 IC50 = 244.0 nM 6.61
CHEMBL1762704 IC50 = 295.0 nM 6.53
CHEMBL1762696 IC50 = 301.0 nM 6.52
CHEMBL1762706 IC50 = 330.0 nM 6.48
CHEMBL1762693 IC50 = 530.0 nM 6.28
CHEMBL1762695 IC50 = 640.0 nM 6.19
CHEMBL1762697 IC50 = 758.0 nM 6.12
CHEMBL1762694 IC50 = 8060.0 nM 5.09