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Assay Detail

CHEMBL1908835

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Binding
Binding constant for STK33 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

Serine/threonine-protein kinase 33 (CHEMBL6005)
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 6.45 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.74
CHEMBL509032 TAE-684 1 8.49
CHEMBL535 SUNITINIB 4.0 1 7.77
CHEMBL603469 LESTAURTINIB 3.0 1 7.58
CHEMBL288441 BOSUTINIB 4.0 1 7.43
CHEMBL464552 1 7.16
CHEMBL1230609 FORETINIB 2.0 1 7.01
CHEMBL1721885 SU-014813 2.0 1 6.89
CHEMBL1908397 KW-2449 1.0 1 6.85
CHEMBL608533 MIDOSTAURIN 4.0 1 6.72
CHEMBL379218 1 6.66
CHEMBL1287853 FEDRATINIB 4.0 1 6.66
CHEMBL491473 CEDIRANIB 3.0 1 6.27
CHEMBL1908395 1 6.11
CHEMBL450786 PHA-665752 1 6.08
CHEMBL180022 NERATINIB 4.0 1 6.03
CHEMBL475251 R-406 2.0 1 6.01
CHEMBL513909 BI-2536 2.0 1 5.96
CHEMBL502835 NINTEDANIB 4.0 1 5.96
CHEMBL574738 AST-487 1.0 1 5.92
CHEMBL24828 VANDETANIB 4.0 1 5.85
CHEMBL428690 ALVOCIDIB 3.0 1 5.77
CHEMBL1336 SORAFENIB 4.0 1 5.62
CHEMBL91829 RUBOXISTAURIN 3.0 1 5.58
CHEMBL377300 BRIVANIB 3.0 1 5.50
CHEMBL223360 LINIFANIB 3.0 1 5.42
CHEMBL1241674 1 5.35
CHEMBL300138 ENZASTAURIN 3.0 1 5.31
CHEMBL939 GEFITINIB 4.0 1 -
CHEMBL608154 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE Kd = 1.8 nM 8.74
CHEMBL509032 TAE-684 Kd = 3.2 nM 8.49
CHEMBL535 SUNITINIB Kd = 17.0 nM 7.77
CHEMBL603469 LESTAURTINIB Kd = 26.0 nM 7.58
CHEMBL288441 BOSUTINIB Kd = 37.0 nM 7.43
CHEMBL464552 Kd = 70.0 nM 7.16
CHEMBL1230609 FORETINIB Kd = 98.0 nM 7.01
CHEMBL1721885 SU-014813 Kd = 130.0 nM 6.89
CHEMBL1908397 KW-2449 Kd = 140.0 nM 6.85
CHEMBL608533 MIDOSTAURIN Kd = 190.0 nM 6.72
CHEMBL379218 Kd = 220.0 nM 6.66
CHEMBL1287853 FEDRATINIB Kd = 220.0 nM 6.66
CHEMBL491473 CEDIRANIB Kd = 540.0 nM 6.27
CHEMBL1908395 Kd = 780.0 nM 6.11
CHEMBL450786 PHA-665752 Kd = 840.0 nM 6.08
CHEMBL180022 NERATINIB Kd = 940.0 nM 6.03
CHEMBL475251 R-406 Kd = 970.0 nM 6.01
CHEMBL513909 BI-2536 Kd = 1100.0 nM 5.96
CHEMBL502835 NINTEDANIB Kd = 1100.0 nM 5.96
CHEMBL574738 AST-487 Kd = 1200.0 nM 5.92
CHEMBL24828 VANDETANIB Kd = 1400.0 nM 5.85
CHEMBL428690 ALVOCIDIB Kd = 1700.0 nM 5.77
CHEMBL1336 SORAFENIB Kd = 2400.0 nM 5.62
CHEMBL91829 RUBOXISTAURIN Kd = 2600.0 nM 5.58
CHEMBL377300 BRIVANIB Kd = 3200.0 nM 5.50
CHEMBL223360 LINIFANIB Kd = 3800.0 nM 5.42
CHEMBL1241674 Kd = 4500.0 nM 5.35
CHEMBL300138 ENZASTAURIN Kd = 4900.0 nM 5.31
CHEMBL386051 Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -
CHEMBL1908396 Kd > 10000.0 nM -
CHEMBL445813 AT-7519 Kd > 10000.0 nM -
CHEMBL494089 GSK-690693 Kd > 10000.0 nM -
CHEMBL259084 MLN-8054 Kd > 10000.0 nM -
CHEMBL255863 NILOTINIB Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL1908391 MASITINIB Kd > 10000.0 nM -
CHEMBL1236107 SGX-523 Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL1908394 GSK-461364 Kd > 10000.0 nM -
CHEMBL31965 CANERTINIB Kd > 10000.0 nM -
CHEMBL522892 DOVITINIB Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL10 SB-203580 Kd > 10000.0 nM -
CHEMBL477772 PAZOPANIB Kd > 10000.0 nM -
CHEMBL576982 QUIZARTINIB Kd > 10000.0 nM -
CHEMBL1289926 AXITINIB Kd > 10000.0 nM -
CHEMBL608154 Kd > 10000.0 nM -
CHEMBL939 GEFITINIB Kd > 10000.0 nM -