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Assay Detail

CHEMBL759509

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Functional
Antagonist activity against recombinant human P2X purinoceptor 1 (P2X1 )
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

P2X purinoceptor 1 (CHEMBL2094)
Type SINGLE PROTEIN
Organism Homo sapiens

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 11 6.61 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339386 1 8.70
CHEMBL1163419 TNP-ATP 1 8.22
CHEMBL336208 1 7.27
CHEMBL14249 ADENOSINE TRIPHOSPHATE 2.0 1 7.25
CHEMBL339385 DIADENOSINE TETRAPHOSPHATE 1 6.74
CHEMBL132722 DIPHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER 1 6.70
CHEMBL129841 1 5.94
CHEMBL133463 PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER 1 5.70
CHEMBL131890 ATPGAMMAS 1 5.64
CHEMBL335206 1 5.60
CHEMBL14830 ADENOSINE DIPHOSPHATE 0.5 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339386 EC50 = 2.0 nM 8.70
CHEMBL1163419 TNP-ATP EC50 = 6.0 nM 8.22
CHEMBL336208 EC50 = 54.0 nM 7.27
CHEMBL14249 ADENOSINE TRIPHOSPHATE EC50 = 56.0 nM 7.25
CHEMBL339385 DIADENOSINE TETRAPHOSPHATE EC50 = 182.0 nM 6.74
CHEMBL132722 DIPHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER EC50 = 200.0 nM 6.70
CHEMBL129841 EC50 = 1150.0 nM 5.94
CHEMBL133463 PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER EC50 = 2000.0 nM 5.70
CHEMBL131890 ATPGAMMAS EC50 = 2300.0 nM 5.64
CHEMBL335206 EC50 = 2500.0 nM 5.60
CHEMBL14830 ADENOSINE DIPHOSPHATE EC50 = 10000.0 nM 5.00