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Assay Detail

CHEMBL1908537

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Binding
Binding constant for AXL 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

Tyrosine-protein kinase receptor UFO (CHEMBL4895)
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 6.67 10.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230609 FORETINIB 2.0 1 10.03
CHEMBL1908395 1 8.28
CHEMBL388978 STAUROSPORINE 1 8.17
CHEMBL601719 CRIZOTINIB 4.0 1 8.11
CHEMBL535 SUNITINIB 4.0 1 8.05
CHEMBL502835 NINTEDANIB 4.0 1 7.92
CHEMBL509032 TAE-684 1 7.92
CHEMBL603469 LESTAURTINIB 3.0 1 7.46
CHEMBL288441 BOSUTINIB 4.0 1 7.28
CHEMBL475251 R-406 2.0 1 7.09
CHEMBL1721885 SU-014813 2.0 1 7.08
CHEMBL450786 PHA-665752 1 6.96
CHEMBL1908396 1 6.85
CHEMBL1287853 FEDRATINIB 4.0 1 6.80
CHEMBL1908397 KW-2449 1.0 1 6.75
CHEMBL180022 NERATINIB 4.0 1 6.72
CHEMBL572878 TOZASERTIB 2.0 1 6.68
CHEMBL24828 VANDETANIB 4.0 1 6.60
CHEMBL464552 1 6.52
CHEMBL223360 LINIFANIB 3.0 1 6.47
CHEMBL215152 DEFOSBARASERTIB 2.0 1 6.41
CHEMBL1289926 AXITINIB 4.0 1 6.38
CHEMBL259084 MLN-8054 1.0 1 6.36
CHEMBL491473 CEDIRANIB 3.0 1 6.31
CHEMBL574738 AST-487 1.0 1 6.24
CHEMBL608533 MIDOSTAURIN 4.0 1 6.21
CHEMBL1241674 1 5.92
CHEMBL939 GEFITINIB 4.0 1 5.75
CHEMBL300138 ENZASTAURIN 3.0 1 5.48
CHEMBL428690 ALVOCIDIB 3.0 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230609 FORETINIB Kd = 0.093 nM 10.03
CHEMBL1908395 Kd = 5.3 nM 8.28
CHEMBL388978 STAUROSPORINE Kd = 6.8 nM 8.17
CHEMBL601719 CRIZOTINIB Kd = 7.8 nM 8.11
CHEMBL535 SUNITINIB Kd = 9.0 nM 8.05
CHEMBL502835 NINTEDANIB Kd = 12.0 nM 7.92
CHEMBL509032 TAE-684 Kd = 12.0 nM 7.92
CHEMBL603469 LESTAURTINIB Kd = 35.0 nM 7.46
CHEMBL288441 BOSUTINIB Kd = 52.0 nM 7.28
CHEMBL475251 R-406 Kd = 82.0 nM 7.09
CHEMBL1721885 SU-014813 Kd = 84.0 nM 7.08
CHEMBL450786 PHA-665752 Kd = 110.0 nM 6.96
CHEMBL1908396 Kd = 140.0 nM 6.85
CHEMBL1287853 FEDRATINIB Kd = 160.0 nM 6.80
CHEMBL1908397 KW-2449 Kd = 180.0 nM 6.75
CHEMBL180022 NERATINIB Kd = 190.0 nM 6.72
CHEMBL572878 TOZASERTIB Kd = 210.0 nM 6.68
CHEMBL24828 VANDETANIB Kd = 250.0 nM 6.60
CHEMBL464552 Kd = 300.0 nM 6.52
CHEMBL223360 LINIFANIB Kd = 340.0 nM 6.47
CHEMBL215152 DEFOSBARASERTIB Kd = 390.0 nM 6.41
CHEMBL1289926 AXITINIB Kd = 420.0 nM 6.38
CHEMBL259084 MLN-8054 Kd = 440.0 nM 6.36
CHEMBL491473 CEDIRANIB Kd = 490.0 nM 6.31
CHEMBL574738 AST-487 Kd = 570.0 nM 6.24
CHEMBL608533 MIDOSTAURIN Kd = 620.0 nM 6.21
CHEMBL1241674 Kd = 1200.0 nM 5.92
CHEMBL939 GEFITINIB Kd = 1800.0 nM 5.75
CHEMBL300138 ENZASTAURIN Kd = 3300.0 nM 5.48
CHEMBL428690 ALVOCIDIB Kd = 3500.0 nM 5.46
CHEMBL522892 DOVITINIB Kd = 3800.0 nM 5.42
CHEMBL553 ERLOTINIB Kd = 4000.0 nM 5.40
CHEMBL1336 SORAFENIB Kd = 4500.0 nM 5.35
CHEMBL1173655 AFATINIB Kd = 5300.0 nM 5.28
CHEMBL31965 CANERTINIB Kd = 5700.0 nM 5.24
CHEMBL124660 TANDUTINIB Kd = 6300.0 nM 5.20
CHEMBL554 LAPATINIB Kd > 10000.0 nM -
CHEMBL10 SB-203580 Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL386051 Kd > 10000.0 nM -
CHEMBL119385 NEFLAMAPIMOD Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL445813 AT-7519 Kd > 10000.0 nM -
CHEMBL255863 NILOTINIB Kd > 10000.0 nM -
CHEMBL1236107 SGX-523 Kd > 10000.0 nM -
CHEMBL494089 GSK-690693 Kd > 10000.0 nM -
CHEMBL1908394 GSK-461364 Kd > 10000.0 nM -
CHEMBL477772 PAZOPANIB Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -