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Assay Detail

CHEMBL1908472

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Binding
Binding constant for STK16 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 16 (CHEMBL3938)
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 6.51 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475251 R-406 2.0 1 8.77
CHEMBL1287853 FEDRATINIB 4.0 1 8.18
CHEMBL1908395 1 7.75
CHEMBL502835 NINTEDANIB 4.0 1 7.75
CHEMBL603469 LESTAURTINIB 3.0 1 7.72
CHEMBL1908397 KW-2449 1.0 1 7.54
CHEMBL535 SUNITINIB 4.0 1 6.60
CHEMBL388978 STAUROSPORINE 1 6.57
CHEMBL608533 MIDOSTAURIN 4.0 1 6.55
CHEMBL477772 PAZOPANIB 4.0 1 6.44
CHEMBL1289926 AXITINIB 4.0 1 6.43
CHEMBL1789941 RUXOLITINIB 4.0 1 6.31
CHEMBL230011 TG100-115 2.0 1 6.27
CHEMBL572878 TOZASERTIB 2.0 1 6.21
CHEMBL1721885 SU-014813 2.0 1 6.14
CHEMBL509032 TAE-684 1 6.10
CHEMBL513909 BI-2536 2.0 1 5.96
CHEMBL521851 PICTILISIB 2.0 1 5.96
CHEMBL522892 DOVITINIB 3.0 1 5.82
CHEMBL1230020 PLX-4720 1 5.72
CHEMBL300138 ENZASTAURIN 3.0 1 5.60
CHEMBL1241674 1 5.40
CHEMBL450786 PHA-665752 1 5.32
CHEMBL464552 1 5.14
CHEMBL119385 NEFLAMAPIMOD 2.0 1 -
CHEMBL1908394 GSK-461364 1.0 1 -
CHEMBL572881 MOTESANIB 3.0 1 -
CHEMBL10 SB-203580 1 -
CHEMBL124660 TANDUTINIB 2.0 1 -
CHEMBL1236107 SGX-523 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475251 R-406 Kd = 1.7 nM 8.77
CHEMBL1287853 FEDRATINIB Kd = 6.6 nM 8.18
CHEMBL502835 NINTEDANIB Kd = 18.0 nM 7.75
CHEMBL1908395 Kd = 18.0 nM 7.75
CHEMBL603469 LESTAURTINIB Kd = 19.0 nM 7.72
CHEMBL1908397 KW-2449 Kd = 29.0 nM 7.54
CHEMBL535 SUNITINIB Kd = 250.0 nM 6.60
CHEMBL388978 STAUROSPORINE Kd = 270.0 nM 6.57
CHEMBL608533 MIDOSTAURIN Kd = 280.0 nM 6.55
CHEMBL477772 PAZOPANIB Kd = 360.0 nM 6.44
CHEMBL1289926 AXITINIB Kd = 370.0 nM 6.43
CHEMBL1789941 RUXOLITINIB Kd = 490.0 nM 6.31
CHEMBL230011 TG100-115 Kd = 540.0 nM 6.27
CHEMBL572878 TOZASERTIB Kd = 610.0 nM 6.21
CHEMBL1721885 SU-014813 Kd = 730.0 nM 6.14
CHEMBL509032 TAE-684 Kd = 800.0 nM 6.10
CHEMBL513909 BI-2536 Kd = 1100.0 nM 5.96
CHEMBL521851 PICTILISIB Kd = 1100.0 nM 5.96
CHEMBL522892 DOVITINIB Kd = 1500.0 nM 5.82
CHEMBL1230020 PLX-4720 Kd = 1900.0 nM 5.72
CHEMBL300138 ENZASTAURIN Kd = 2500.0 nM 5.60
CHEMBL1241674 Kd = 4000.0 nM 5.40
CHEMBL450786 PHA-665752 Kd = 4800.0 nM 5.32
CHEMBL464552 Kd = 7300.0 nM 5.14
CHEMBL255863 NILOTINIB Kd > 10000.0 nM -
CHEMBL1336 SORAFENIB Kd > 10000.0 nM -
CHEMBL31965 CANERTINIB Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL215152 DEFOSBARASERTIB Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -
CHEMBL180022 NERATINIB Kd > 10000.0 nM -
CHEMBL386051 Kd > 10000.0 nM -
CHEMBL428690 ALVOCIDIB Kd > 10000.0 nM -
CHEMBL221959 TOFACITINIB Kd > 10000.0 nM -
CHEMBL941 IMATINIB Kd > 10000.0 nM -
CHEMBL1614701 SELUMETINIB Kd > 10000.0 nM -
CHEMBL601719 CRIZOTINIB Kd > 10000.0 nM -
CHEMBL494089 GSK-690693 Kd > 10000.0 nM -
CHEMBL445813 AT-7519 Kd > 10000.0 nM -
CHEMBL288441 BOSUTINIB Kd > 10000.0 nM -
CHEMBL259084 MLN-8054 Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL574738 AST-487 Kd > 10000.0 nM -
CHEMBL608154 Kd > 10000.0 nM -
CHEMBL1236107 SGX-523 Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -
CHEMBL10 SB-203580 Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL1908394 GSK-461364 Kd > 10000.0 nM -
CHEMBL119385 NEFLAMAPIMOD Kd > 10000.0 nM -