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Assay Detail

CHEMBL930506

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

Binding
Binding affinity to human P2Y1 receptor
46
Total Activities
46
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

P2Y1 receptor antagonists as novel antithrombotic agents.
Pfefferkorn JA, Choi C, Winters T, Kennedy R, Chi L, Perrin LA, Lu G, Ping YW, McClanahan T, Schroeder R, Leininger MT, Geyer A, Schefzick S, Atherton J.
Bioorg Med Chem Lett (2008) 18 : 3338 -3343
PubMed 18445527 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 6.71 9.11
Kd 1 6.96 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL444278 1 9.11
CHEMBL255724 1 8.00
CHEMBL255095 1 7.70
CHEMBL256088 1 7.52
CHEMBL256141 1 7.52
CHEMBL258406 1 7.30
CHEMBL257559 1 7.22
CHEMBL402837 1 7.22
CHEMBL255307 1 7.16
CHEMBL255306 1 7.05
CHEMBL256776 1 7.00
CHEMBL129841 1 6.96
CHEMBL255094 1 6.92
CHEMBL256089 1 6.92
CHEMBL403879 1 6.89
CHEMBL402563 1 6.89
CHEMBL255308 1 6.85
CHEMBL255728 1 6.82
CHEMBL255310 1 6.75
CHEMBL404869 1 6.70
CHEMBL257560 1 6.60
CHEMBL255726 1 6.60
CHEMBL257378 1 6.57
CHEMBL403555 1 6.54
CHEMBL401657 1 6.25
CHEMBL402597 1 6.16
CHEMBL255447 1 6.12
CHEMBL255727 1 6.02
CHEMBL258235 1 5.92
CHEMBL258407 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL444278 Ki = 0.78 nM 9.11
CHEMBL255724 Ki = 10.0 nM 8.00
CHEMBL255095 Ki = 20.0 nM 7.70
CHEMBL256088 Ki = 30.0 nM 7.52
CHEMBL256141 Ki = 30.0 nM 7.52
CHEMBL258406 Ki = 50.0 nM 7.30
CHEMBL257559 Ki = 60.0 nM 7.22
CHEMBL402837 Ki = 60.0 nM 7.22
CHEMBL255307 Ki = 70.0 nM 7.16
CHEMBL255306 Ki = 90.0 nM 7.05
CHEMBL256776 Ki = 100.0 nM 7.00
CHEMBL129841 Kd = 109.0 nM 6.96
CHEMBL256089 Ki = 120.0 nM 6.92
CHEMBL255094 Ki = 120.0 nM 6.92
CHEMBL402563 Ki = 130.0 nM 6.89
CHEMBL403879 Ki = 130.0 nM 6.89
CHEMBL255308 Ki = 140.0 nM 6.85
CHEMBL255728 Ki = 150.0 nM 6.82
CHEMBL255310 Ki = 180.0 nM 6.75
CHEMBL404869 Ki = 200.0 nM 6.70
CHEMBL257560 Ki = 250.0 nM 6.60
CHEMBL255726 Ki = 250.0 nM 6.60
CHEMBL257378 Ki = 270.0 nM 6.57
CHEMBL403555 Ki = 290.0 nM 6.54
CHEMBL401657 Ki = 560.0 nM 6.25
CHEMBL402597 Ki = 700.0 nM 6.16
CHEMBL255447 Ki = 760.0 nM 6.12
CHEMBL255727 Ki = 960.0 nM 6.02
CHEMBL258235 Ki = 1200.0 nM 5.92
CHEMBL258407 Ki = 1800.0 nM 5.75
CHEMBL430029 Ki = 2700.0 nM 5.57
CHEMBL255505 Ki = 4900.0 nM 5.31
CHEMBL255093 Ki = 5200.0 nM 5.28
CHEMBL255278 Ki = 7200.0 nM 5.14
CHEMBL256944 Ki > 10000.0 nM -
CHEMBL256943 Ki > 10000.0 nM -
CHEMBL258429 Ki > 10000.0 nM -
CHEMBL428431 Ki > 10000.0 nM -
CHEMBL257136 Ki > 10000.0 nM -
CHEMBL258234 Ki > 10000.0 nM -
CHEMBL255454 Ki > 10000.0 nM -
CHEMBL255455 Ki > 10000.0 nM -
CHEMBL403824 Ki > 10000.0 nM -
CHEMBL402793 Ki > 10000.0 nM -
CHEMBL255506 Ki > 10000.0 nM -
CHEMBL255252 Ki > 10000.0 nM -