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Assay Detail

CHEMBL1908541

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Binding
Binding constant for CDK2 kinase domain
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 2 (CHEMBL301)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Comprehensive analysis of kinase inhibitor selectivity.
Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP.
Nat Biotechnol (2011) 29 : 1046 -1051
PubMed 22037378 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 72 6.72 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384304 RG-547 2.0 1 9.28
CHEMBL388978 STAUROSPORINE 1 8.15
CHEMBL603469 LESTAURTINIB 3.0 1 7.70
CHEMBL445813 AT-7519 2.0 1 7.52
CHEMBL296468 BMS-387032 1.0 1 7.16
CHEMBL574738 AST-487 1.0 1 6.35
CHEMBL428690 ALVOCIDIB 3.0 1 6.26
CHEMBL502835 NINTEDANIB 4.0 1 5.85
CHEMBL300138 ENZASTAURIN 3.0 1 5.30
CHEMBL509032 TAE-684 1 5.28
CHEMBL1336 SORAFENIB 4.0 1 5.06
CHEMBL475251 R-406 2.0 1 -
CHEMBL1236107 SGX-523 1.0 1 -
CHEMBL124660 TANDUTINIB 2.0 1 -
CHEMBL477772 PAZOPANIB 4.0 1 -
CHEMBL572881 MOTESANIB 3.0 1 -
CHEMBL10 SB-203580 1 -
CHEMBL386051 1 -
CHEMBL521851 PICTILISIB 2.0 1 -
CHEMBL91829 RUBOXISTAURIN 3.0 1 -
CHEMBL119385 NEFLAMAPIMOD 2.0 1 -
CHEMBL522892 DOVITINIB 3.0 1 -
CHEMBL377300 BRIVANIB 3.0 1 -
CHEMBL939 GEFITINIB 4.0 1 -
CHEMBL180022 NERATINIB 4.0 1 -
CHEMBL1289926 AXITINIB 4.0 1 -
CHEMBL105442 CI-1040 2.0 1 -
CHEMBL464552 1 -
CHEMBL608154 1 -
CHEMBL576982 QUIZARTINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384304 RG-547 Kd = 0.53 nM 9.28
CHEMBL388978 STAUROSPORINE Kd = 7.0 nM 8.15
CHEMBL603469 LESTAURTINIB Kd = 20.0 nM 7.70
CHEMBL445813 AT-7519 Kd = 30.0 nM 7.52
CHEMBL296468 BMS-387032 Kd = 69.0 nM 7.16
CHEMBL574738 AST-487 Kd = 450.0 nM 6.35
CHEMBL428690 ALVOCIDIB Kd = 550.0 nM 6.26
CHEMBL502835 NINTEDANIB Kd = 1400.0 nM 5.85
CHEMBL300138 ENZASTAURIN Kd = 5000.0 nM 5.30
CHEMBL509032 TAE-684 Kd = 5200.0 nM 5.28
CHEMBL1336 SORAFENIB Kd = 8700.0 nM 5.06
CHEMBL259084 MLN-8054 Kd > 10000.0 nM -
CHEMBL450786 PHA-665752 Kd > 10000.0 nM -
CHEMBL288441 BOSUTINIB Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL494089 GSK-690693 Kd > 10000.0 nM -
CHEMBL255863 NILOTINIB Kd > 10000.0 nM -
CHEMBL215152 DEFOSBARASERTIB Kd > 10000.0 nM -
CHEMBL31965 CANERTINIB Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL535 SUNITINIB Kd > 10000.0 nM -
CHEMBL553 ERLOTINIB Kd > 10000.0 nM -
CHEMBL1173655 AFATINIB Kd > 10000.0 nM -
CHEMBL230011 TG100-115 Kd > 10000.0 nM -
CHEMBL608533 MIDOSTAURIN Kd > 10000.0 nM -
CHEMBL1908395 Kd > 10000.0 nM -
CHEMBL573339 PI-103 Kd > 10000.0 nM -
CHEMBL5416410 DASATINIB Kd > 10000.0 nM -
CHEMBL513909 BI-2536 Kd > 10000.0 nM -
CHEMBL1908396 Kd > 10000.0 nM -
CHEMBL119385 NEFLAMAPIMOD Kd > 10000.0 nM -
CHEMBL576982 QUIZARTINIB Kd > 10000.0 nM -
CHEMBL608154 Kd > 10000.0 nM -
CHEMBL464552 Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -
CHEMBL1289926 AXITINIB Kd > 10000.0 nM -
CHEMBL180022 NERATINIB Kd > 10000.0 nM -
CHEMBL939 GEFITINIB Kd > 10000.0 nM -
CHEMBL377300 BRIVANIB Kd > 10000.0 nM -
CHEMBL522892 DOVITINIB Kd > 10000.0 nM -
CHEMBL1908394 GSK-461364 Kd > 10000.0 nM -
CHEMBL91829 RUBOXISTAURIN Kd > 10000.0 nM -
CHEMBL521851 PICTILISIB Kd > 10000.0 nM -
CHEMBL386051 Kd > 10000.0 nM -
CHEMBL10 SB-203580 Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL477772 PAZOPANIB Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -
CHEMBL1236107 SGX-523 Kd > 10000.0 nM -
CHEMBL475251 R-406 Kd > 10000.0 nM -