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Assay Detail

CHEMBL750155

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

Binding
Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.
Ravi RG, Kim HS, Servos J, Zimmermann H, Lee K, Maddileti S, Boyer JL, Harden TK, Jacobson KA.
J Med Chem (2002) 45 : 2090 -2100
PubMed 11985476 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 7.26 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2373948 1 9.40
CHEMBL435402 1 8.19
CHEMBL2373323 1 8.15
CHEMBL2373377 1 8.05
CHEMBL2373389 1 7.64
CHEMBL2373324 1 7.48
CHEMBL336208 1 7.47
CHEMBL302077 1 7.28
CHEMBL2373325 1 6.80
CHEMBL2373947 1 6.23
CHEMBL1368696 1 6.11
CHEMBL14249 ADENOSINE TRIPHOSPHATE 2.0 1 5.82
CHEMBL2373945 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2373948 EC50 = 0.4 nM 9.40
CHEMBL435402 EC50 = 6.4 nM 8.19
CHEMBL2373323 EC50 = 7.0 nM 8.15
CHEMBL2373377 EC50 = 9.0 nM 8.05
CHEMBL2373389 EC50 = 23.0 nM 7.64
CHEMBL2373324 EC50 = 33.0 nM 7.48
CHEMBL336208 EC50 = 34.0 nM 7.47
CHEMBL302077 EC50 = 52.0 nM 7.28
CHEMBL2373325 EC50 = 158.0 nM 6.80
CHEMBL2373947 EC50 = 590.0 nM 6.23
CHEMBL1368696 EC50 = 770.0 nM 6.11
CHEMBL14249 ADENOSINE TRIPHOSPHATE EC50 = 1500.0 nM 5.82
CHEMBL2373945 EC50 = 1890.0 nM 5.72