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Assay Detail

CHEMBL3267606

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

Binding
Displacement of [33P]2-MeS-ADP from human cloned P2Y1 receptor expressed in HEK293 cells by SPA analysis
23
Total Activities
23
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

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

Publication

2-Amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists.
Hu CH, Qiao JX, Han Y, Wang TC, Hua J, Price LA, Wu Q, Shen H, Huang CS, Rehfuss R, Wexler RR, Lam PY.
Bioorg Med Chem Lett (2014) 24 : 2481 -2485
PubMed 24767843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.77 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3263070 1 8.28
CHEMBL3263058 1 8.22
CHEMBL3263059 1 8.21
CHEMBL3263075 1 8.19
CHEMBL3263076 1 8.18
CHEMBL2393201 1 8.15
CHEMBL3263056 1 8.10
CHEMBL3263069 1 8.10
CHEMBL3263057 1 8.02
CHEMBL3263068 1 8.01
CHEMBL2401864 1 7.92
CHEMBL3263071 1 7.89
CHEMBL3263074 1 7.89
CHEMBL3263066 1 7.80
CHEMBL3263073 1 7.80
CHEMBL3263062 1 7.77
CHEMBL3263061 1 7.70
CHEMBL3263067 1 7.58
CHEMBL3263072 1 7.55
CHEMBL3263065 1 7.31
CHEMBL3263060 1 7.18
CHEMBL3263063 1 6.46
CHEMBL3263064 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3263070 Ki = 5.3 nM 8.28
CHEMBL3263058 Ki = 6.0 nM 8.22
CHEMBL3263059 Ki = 6.2 nM 8.21
CHEMBL3263075 Ki = 6.5 nM 8.19
CHEMBL3263076 Ki = 6.6 nM 8.18
CHEMBL2393201 Ki = 7.0 nM 8.15
CHEMBL3263056 Ki = 8.0 nM 8.10
CHEMBL3263069 Ki = 8.0 nM 8.10
CHEMBL3263057 Ki = 9.6 nM 8.02
CHEMBL3263068 Ki = 9.7 nM 8.01
CHEMBL2401864 Ki = 12.0 nM 7.92
CHEMBL3263071 Ki = 13.0 nM 7.89
CHEMBL3263074 Ki = 13.0 nM 7.89
CHEMBL3263066 Ki = 16.0 nM 7.80
CHEMBL3263073 Ki = 16.0 nM 7.80
CHEMBL3263062 Ki = 17.0 nM 7.77
CHEMBL3263061 Ki = 20.0 nM 7.70
CHEMBL3263067 Ki = 26.0 nM 7.58
CHEMBL3263072 Ki = 28.0 nM 7.55
CHEMBL3263065 Ki = 49.0 nM 7.31
CHEMBL3263060 Ki = 66.0 nM 7.18
CHEMBL3263063 Ki = 343.0 nM 6.46
CHEMBL3263064 Ki = 511.0 nM 6.29