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Assay Detail

CHEMBL1064501

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

Binding
Inhibition of human P2Y12 receptor expressed in CHO cells
84
Total Activities
84
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

P2Y purinoceptor 12 (CHEMBL2001)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Part II: piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation.
Parlow JJ, Burney MW, Case BL, Girard TJ, Hall KA, Harris PK, Hiebsch RR, Huff RM, Lachance RM, Mischke DA, Rapp SR, Woerndle RS, Ennis MD.
Bioorg Med Chem Lett (2010) 20 : 1388 -1394
PubMed 20097563 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 84 8.27 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL601696 1 9.24
CHEMBL601489 1 9.19
CHEMBL570295 1 9.17
CHEMBL601695 1 9.10
CHEMBL601698 1 9.01
CHEMBL601903 1 8.96
CHEMBL601692 1 8.96
CHEMBL601905 1 8.92
CHEMBL601485 1 8.85
CHEMBL601478 1 8.82
CHEMBL589804 1 8.82
CHEMBL589519 1 8.82
CHEMBL590260 1 8.77
CHEMBL601483 1 8.77
CHEMBL590008 1 8.77
CHEMBL590146 1 8.77
CHEMBL589335 1 8.72
CHEMBL601486 1 8.70
CHEMBL589901 1 8.70
CHEMBL601906 1 8.68
CHEMBL590194 1 8.60
CHEMBL601484 1 8.59
CHEMBL590004 1 8.59
CHEMBL602111 1 8.55
CHEMBL601907 1 8.55
CHEMBL589824 1 8.55
CHEMBL589584 1 8.49
CHEMBL601487 1 8.48
CHEMBL590069 1 8.46
CHEMBL589520 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL601696 Ki = 0.58 nM 9.24
CHEMBL601489 Ki = 0.64 nM 9.19
CHEMBL570295 Ki = 0.68 nM 9.17
CHEMBL601695 Ki = 0.79 nM 9.10
CHEMBL601698 Ki = 0.98 nM 9.01
CHEMBL601903 Ki = 1.1 nM 8.96
CHEMBL601692 Ki = 1.1 nM 8.96
CHEMBL601905 Ki = 1.2 nM 8.92
CHEMBL601485 Ki = 1.4 nM 8.85
CHEMBL601478 Ki = 1.5 nM 8.82
CHEMBL589804 Ki = 1.5 nM 8.82
CHEMBL589519 Ki = 1.5 nM 8.82
CHEMBL590008 Ki = 1.7 nM 8.77
CHEMBL590260 Ki = 1.7 nM 8.77
CHEMBL601483 Ki = 1.7 nM 8.77
CHEMBL590146 Ki = 1.7 nM 8.77
CHEMBL589335 Ki = 1.9 nM 8.72
CHEMBL601486 Ki = 2.0 nM 8.70
CHEMBL589901 Ki = 2.0 nM 8.70
CHEMBL601906 Ki = 2.1 nM 8.68
CHEMBL590194 Ki = 2.5 nM 8.60
CHEMBL601484 Ki = 2.6 nM 8.59
CHEMBL590004 Ki = 2.6 nM 8.59
CHEMBL589824 Ki = 2.8 nM 8.55
CHEMBL602111 Ki = 2.8 nM 8.55
CHEMBL601907 Ki = 2.8 nM 8.55
CHEMBL589584 Ki = 3.2 nM 8.49
CHEMBL601487 Ki = 3.3 nM 8.48
CHEMBL590069 Ki = 3.5 nM 8.46
CHEMBL589520 Ki = 3.8 nM 8.42
CHEMBL589518 Ki = 4.0 nM 8.40
CHEMBL589889 Ki = 4.0 nM 8.40
CHEMBL589971 Ki = 4.0 nM 8.40
CHEMBL601697 Ki = 4.3 nM 8.37
CHEMBL590007 Ki = 4.5 nM 8.35
CHEMBL601904 Ki = 4.8 nM 8.32
CHEMBL601910 Ki = 4.9 nM 8.31
CHEMBL590114 Ki = 5.0 nM 8.30
CHEMBL602109 Ki = 5.2 nM 8.28
CHEMBL590261 Ki = 5.5 nM 8.26
CHEMBL601271 Ki = 5.5 nM 8.26
CHEMBL602112 Ki = 5.9 nM 8.23
CHEMBL602108 Ki = 5.9 nM 8.23
CHEMBL589828 Ki = 6.0 nM 8.22
CHEMBL590009 Ki = 6.3 nM 8.20
CHEMBL589697 Ki = 6.3 nM 8.20
CHEMBL589897 Ki = 6.5 nM 8.19
CHEMBL590005 Ki = 6.5 nM 8.19
CHEMBL601488 Ki = 7.1 nM 8.15
CHEMBL601273 Ki = 7.3 nM 8.14