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Assay Detail

CHEMBL3107657

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

Binding
Antagonist activity at P2X1 receptor in HEK293 cells assessed as alpha, beta-methylene ATP-induced calcium flux by FLIPR assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.
Qiao JX, Wang TC, Ruel R, Thibeault C, L'Heureux A, Schumacher WA, Spronk SA, Hiebert S, Bouthillier G, Lloyd J, Pi Z, Schnur DM, Abell LM, Hua J, Price LA, Liu E, Wu Q, Steinbacher TE, Bostwick JS, Chang M, Zheng J, Gao Q, Ma B, McDonnell PA, Huang CS, Rehfuss R, Wexler RR, Lam PY.
J Med Chem (2013) 56 : 9275 -9295
PubMed 24164581 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.80 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3104636 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3104636 IC50 = 1600.0 nM 5.80