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Assay Detail

CHEMBL1908506

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Binding
Binding constant for MYLK4 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

Myosin light chain kinase family member 4 (CHEMBL5426)
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 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535 SUNITINIB 4.0 1 7.82
CHEMBL603469 LESTAURTINIB 3.0 1 7.54
CHEMBL1721885 SU-014813 2.0 1 7.50
CHEMBL522892 DOVITINIB 3.0 1 7.10
CHEMBL1287853 FEDRATINIB 4.0 1 6.89
CHEMBL1908397 KW-2449 1.0 1 6.77
CHEMBL300138 ENZASTAURIN 3.0 1 6.64
CHEMBL502835 NINTEDANIB 4.0 1 6.36
CHEMBL388978 STAUROSPORINE 1 6.33
CHEMBL608533 MIDOSTAURIN 4.0 1 6.19
CHEMBL249697 BMS-345541 1 6.16
CHEMBL521851 PICTILISIB 2.0 1 6.11
CHEMBL475251 R-406 2.0 1 6.09
CHEMBL1908395 1 6.06
CHEMBL379218 1 5.82
CHEMBL572878 TOZASERTIB 2.0 1 5.66
CHEMBL296468 BMS-387032 1.0 1 5.62
CHEMBL1230020 PLX-4720 1 5.47
CHEMBL10 SB-203580 1 -
CHEMBL572881 MOTESANIB 3.0 1 -
CHEMBL1289926 AXITINIB 4.0 1 -
CHEMBL608154 1 -
CHEMBL384304 RG-547 2.0 1 -
CHEMBL119385 NEFLAMAPIMOD 2.0 1 -
CHEMBL124660 TANDUTINIB 2.0 1 -
CHEMBL464552 1 -
CHEMBL1236107 SGX-523 1.0 1 -
CHEMBL574738 AST-487 1.0 1 -
CHEMBL558752 RAF-265 2.0 1 -
CHEMBL1908394 GSK-461364 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535 SUNITINIB Kd = 15.0 nM 7.82
CHEMBL603469 LESTAURTINIB Kd = 29.0 nM 7.54
CHEMBL1721885 SU-014813 Kd = 32.0 nM 7.50
CHEMBL522892 DOVITINIB Kd = 80.0 nM 7.10
CHEMBL1287853 FEDRATINIB Kd = 130.0 nM 6.89
CHEMBL1908397 KW-2449 Kd = 170.0 nM 6.77
CHEMBL300138 ENZASTAURIN Kd = 230.0 nM 6.64
CHEMBL502835 NINTEDANIB Kd = 440.0 nM 6.36
CHEMBL388978 STAUROSPORINE Kd = 470.0 nM 6.33
CHEMBL608533 MIDOSTAURIN Kd = 640.0 nM 6.19
CHEMBL249697 BMS-345541 Kd = 700.0 nM 6.16
CHEMBL521851 PICTILISIB Kd = 780.0 nM 6.11
CHEMBL475251 R-406 Kd = 810.0 nM 6.09
CHEMBL1908395 Kd = 870.0 nM 6.06
CHEMBL379218 Kd = 1500.0 nM 5.82
CHEMBL572878 TOZASERTIB Kd = 2200.0 nM 5.66
CHEMBL296468 BMS-387032 Kd = 2400.0 nM 5.62
CHEMBL1230020 PLX-4720 Kd = 3400.0 nM 5.47
CHEMBL1789941 RUXOLITINIB Kd > 10000.0 nM -
CHEMBL601719 CRIZOTINIB Kd > 10000.0 nM -
CHEMBL1614701 SELUMETINIB Kd > 10000.0 nM -
CHEMBL450786 PHA-665752 Kd > 10000.0 nM -
CHEMBL941 IMATINIB Kd > 10000.0 nM -
CHEMBL221959 TOFACITINIB Kd > 10000.0 nM -
CHEMBL1230609 FORETINIB Kd > 10000.0 nM -
CHEMBL386051 Kd > 10000.0 nM -
CHEMBL180022 NERATINIB Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -
CHEMBL215152 DEFOSBARASERTIB Kd > 10000.0 nM -
CHEMBL477772 PAZOPANIB Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL31965 CANERTINIB Kd > 10000.0 nM -
CHEMBL445813 AT-7519 Kd > 10000.0 nM -
CHEMBL1336 SORAFENIB Kd > 10000.0 nM -
CHEMBL255863 NILOTINIB Kd > 10000.0 nM -
CHEMBL494089 GSK-690693 Kd > 10000.0 nM -
CHEMBL288441 BOSUTINIB Kd > 10000.0 nM -
CHEMBL259084 MLN-8054 Kd > 10000.0 nM -
CHEMBL1908394 GSK-461364 Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL574738 AST-487 Kd > 10000.0 nM -
CHEMBL1236107 SGX-523 Kd > 10000.0 nM -
CHEMBL464552 Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -
CHEMBL119385 NEFLAMAPIMOD Kd > 10000.0 nM -
CHEMBL384304 RG-547 Kd > 10000.0 nM -
CHEMBL608154 Kd > 10000.0 nM -
CHEMBL1289926 AXITINIB Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL10 SB-203580 Kd > 10000.0 nM -