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Assay Detail

CHEMBL1908745

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Binding
Binding constant for PRKCD 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

Protein kinase C delta type (CHEMBL2996)
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 6.69 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.82
CHEMBL91829 RUBOXISTAURIN 3.0 1 8.44
CHEMBL300138 ENZASTAURIN 3.0 1 7.60
CHEMBL379218 1 7.57
CHEMBL494089 GSK-690693 1.0 1 7.27
CHEMBL603469 LESTAURTINIB 3.0 1 6.62
CHEMBL608533 MIDOSTAURIN 4.0 1 6.50
CHEMBL428690 ALVOCIDIB 3.0 1 6.23
CHEMBL288441 BOSUTINIB 4.0 1 5.80
CHEMBL221959 TOFACITINIB 4.0 1 5.70
CHEMBL1908394 GSK-461364 1.0 1 5.52
CHEMBL509032 TAE-684 1 5.46
CHEMBL475251 R-406 2.0 1 5.39
CHEMBL1336 SORAFENIB 4.0 1 -
CHEMBL1289926 AXITINIB 4.0 1 -
CHEMBL445813 AT-7519 2.0 1 -
CHEMBL10 SB-203580 1 -
CHEMBL105442 CI-1040 2.0 1 -
CHEMBL608154 1 -
CHEMBL939 GEFITINIB 4.0 1 -
CHEMBL377300 BRIVANIB 3.0 1 -
CHEMBL576982 QUIZARTINIB 4.0 1 -
CHEMBL384304 RG-547 2.0 1 -
CHEMBL261849 GW632580X 1 -
CHEMBL521851 PICTILISIB 2.0 1 -
CHEMBL296468 BMS-387032 1.0 1 -
CHEMBL119385 NEFLAMAPIMOD 2.0 1 -
CHEMBL477772 PAZOPANIB 4.0 1 -
CHEMBL223360 LINIFANIB 3.0 1 -
CHEMBL215152 DEFOSBARASERTIB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE Kd = 1.5 nM 8.82
CHEMBL91829 RUBOXISTAURIN Kd = 3.6 nM 8.44
CHEMBL300138 ENZASTAURIN Kd = 25.0 nM 7.60
CHEMBL379218 Kd = 27.0 nM 7.57
CHEMBL494089 GSK-690693 Kd = 54.0 nM 7.27
CHEMBL603469 LESTAURTINIB Kd = 240.0 nM 6.62
CHEMBL608533 MIDOSTAURIN Kd = 320.0 nM 6.50
CHEMBL428690 ALVOCIDIB Kd = 590.0 nM 6.23
CHEMBL288441 BOSUTINIB Kd = 1600.0 nM 5.80
CHEMBL221959 TOFACITINIB Kd = 2000.0 nM 5.70
CHEMBL1908394 GSK-461364 Kd = 3000.0 nM 5.52
CHEMBL509032 TAE-684 Kd = 3500.0 nM 5.46
CHEMBL475251 R-406 Kd = 4100.0 nM 5.39
CHEMBL1236107 SGX-523 Kd > 10000.0 nM -
CHEMBL1789941 RUXOLITINIB Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL522892 DOVITINIB Kd > 10000.0 nM -
CHEMBL255863 NILOTINIB Kd > 10000.0 nM -
CHEMBL259084 MLN-8054 Kd > 10000.0 nM -
CHEMBL31965 CANERTINIB Kd > 10000.0 nM -
CHEMBL574738 AST-487 Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL553 ERLOTINIB Kd > 10000.0 nM -
CHEMBL180022 NERATINIB Kd > 10000.0 nM -
CHEMBL386051 Kd > 10000.0 nM -
CHEMBL1721885 SU-014813 Kd > 10000.0 nM -
CHEMBL941 IMATINIB Kd > 10000.0 nM -
CHEMBL450786 PHA-665752 Kd > 10000.0 nM -
CHEMBL535 SUNITINIB Kd > 10000.0 nM -
CHEMBL1614701 SELUMETINIB Kd > 10000.0 nM -
CHEMBL601719 CRIZOTINIB Kd > 10000.0 nM -
CHEMBL377300 BRIVANIB Kd > 10000.0 nM -
CHEMBL215152 DEFOSBARASERTIB Kd > 10000.0 nM -
CHEMBL223360 LINIFANIB Kd > 10000.0 nM -
CHEMBL477772 PAZOPANIB Kd > 10000.0 nM -
CHEMBL119385 NEFLAMAPIMOD Kd > 10000.0 nM -
CHEMBL296468 BMS-387032 Kd > 10000.0 nM -
CHEMBL521851 PICTILISIB Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL384304 RG-547 Kd > 10000.0 nM -
CHEMBL576982 QUIZARTINIB Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -
CHEMBL939 GEFITINIB Kd > 10000.0 nM -
CHEMBL608154 Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -
CHEMBL10 SB-203580 Kd > 10000.0 nM -
CHEMBL445813 AT-7519 Kd > 10000.0 nM -
CHEMBL1289926 AXITINIB Kd > 10000.0 nM -
CHEMBL1336 SORAFENIB Kd > 10000.0 nM -
CHEMBL464552 Kd > 10000.0 nM -