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Assay Detail

CHEMBL756289

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Functional
Antagonist activity against phospholipase C coupled rat P2Y purinoceptor 12 (P2Y12)
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

P2Y purinoceptor 12 (CHEMBL2188)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Purine and pyrimidine (P2) receptors as drug targets.
Jacobson KA, Jarvis MF, Williams M.
J Med Chem (2002) 45 : 4057 -4093
PubMed 12213051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.80 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336208 1 8.96
CHEMBL223344 RB 2 1 7.60
CHEMBL14830 ADENOSINE DIPHOSPHATE 0.5 1 7.16
CHEMBL335206 1 7.09
CHEMBL131890 ATPGAMMAS 1 5.89
CHEMBL14249 ADENOSINE TRIPHOSPHATE 2.0 1 5.50
CHEMBL265502 SURAMIN 3.0 1 5.40
CHEMBL133463 PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER 1 -
CHEMBL132722 DIPHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER 1 -
CHEMBL3085531 1 -
CHEMBL129841 1 -
CHEMBL69234 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336208 EC50 = 1.1 nM 8.96
CHEMBL223344 RB 2 EC50 = 25.0 nM 7.60
CHEMBL14830 ADENOSINE DIPHOSPHATE EC50 = 69.0 nM 7.16
CHEMBL335206 EC50 = 82.0 nM 7.09
CHEMBL131890 ATPGAMMAS EC50 = 1300.0 nM 5.89
CHEMBL14249 ADENOSINE TRIPHOSPHATE EC50 = 3190.0 nM 5.50
CHEMBL265502 SURAMIN EC50 = 4000.0 nM 5.40
CHEMBL133463 PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER EC50 > 100000.0 nM -
CHEMBL132722 DIPHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER EC50 > 100000.0 nM -
CHEMBL3085531 EC50 > 100000.0 nM -
CHEMBL129841 EC50 > 100000.0 nM -
CHEMBL69234 EC50 > 100000.0 nM -