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Assay Detail

CHEMBL750159

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Functional
Antagonistic activity against P2Y purinoceptor 1
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

P2Y purinoceptor 1 (CHEMBL4315)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.
Kim HS, Ohno M, Xu B, Kim HO, Choi Y, Ji XD, Maddileti S, Marquez VE, Harden TK, Jacobson KA.
J Med Chem (2003) 46 : 4974 -4987
PubMed 14584948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.74 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL444278 1 8.08
CHEMBL146342 1 7.43
CHEMBL2112867 1 7.31
CHEMBL2112864 1 7.28
CHEMBL343651 1 7.06
CHEMBL2112863 1 6.80
CHEMBL2112865 1 6.66
CHEMBL2112868 1 6.45
CHEMBL2112861 1 6.43
CHEMBL356041 1 6.42
CHEMBL2112869 1 6.34
CHEMBL2112866 1 5.73
CHEMBL2112007 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL444278 IC50 = 8.4 nM 8.08
CHEMBL146342 IC50 = 37.0 nM 7.43
CHEMBL2112867 IC50 = 49.0 nM 7.31
CHEMBL2112864 IC50 = 52.0 nM 7.28
CHEMBL343651 IC50 = 87.0 nM 7.06
CHEMBL2112863 IC50 = 157.0 nM 6.80
CHEMBL2112865 IC50 = 221.0 nM 6.66
CHEMBL2112868 IC50 = 356.0 nM 6.45
CHEMBL2112861 IC50 = 367.0 nM 6.43
CHEMBL356041 IC50 = 377.0 nM 6.42
CHEMBL2112869 IC50 = 452.0 nM 6.34
CHEMBL2112866 IC50 = 1870.0 nM 5.73
CHEMBL2112007 IC50 = 2400.0 nM 5.62