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Assay Detail

CHEMBL1908707

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Binding
Binding constant for FER 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 Fer (CHEMBL3982)
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 6.55 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL509032 TAE-684 1 8.85
CHEMBL464552 1 8.03
CHEMBL388978 STAUROSPORINE 1 7.62
CHEMBL603469 LESTAURTINIB 3.0 1 7.55
CHEMBL1721885 SU-014813 2.0 1 7.47
CHEMBL1230609 FORETINIB 2.0 1 7.43
CHEMBL502835 NINTEDANIB 4.0 1 7.14
CHEMBL1908395 1 6.92
CHEMBL475251 R-406 2.0 1 6.89
CHEMBL601719 CRIZOTINIB 4.0 1 6.57
CHEMBL288441 BOSUTINIB 4.0 1 6.44
CHEMBL180022 NERATINIB 4.0 1 6.29
CHEMBL574738 AST-487 1.0 1 6.23
CHEMBL1908397 KW-2449 1.0 1 5.96
CHEMBL1287853 FEDRATINIB 4.0 1 5.96
CHEMBL535 SUNITINIB 4.0 1 5.96
CHEMBL608533 MIDOSTAURIN 4.0 1 5.92
CHEMBL477772 PAZOPANIB 4.0 1 5.57
CHEMBL386051 1 5.46
CHEMBL572878 TOZASERTIB 2.0 1 5.38
CHEMBL259084 MLN-8054 1.0 1 5.36
CHEMBL558752 RAF-265 2.0 1 5.07
CHEMBL1236107 SGX-523 1.0 1 -
CHEMBL576982 QUIZARTINIB 4.0 1 -
CHEMBL124660 TANDUTINIB 2.0 1 -
CHEMBL1614701 SELUMETINIB 4.0 1 -
CHEMBL221959 TOFACITINIB 4.0 1 -
CHEMBL1289926 AXITINIB 4.0 1 -
CHEMBL10 SB-203580 1 -
CHEMBL608154 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL509032 TAE-684 Kd = 1.4 nM 8.85
CHEMBL464552 Kd = 9.3 nM 8.03
CHEMBL388978 STAUROSPORINE Kd = 24.0 nM 7.62
CHEMBL603469 LESTAURTINIB Kd = 28.0 nM 7.55
CHEMBL1721885 SU-014813 Kd = 34.0 nM 7.47
CHEMBL1230609 FORETINIB Kd = 37.0 nM 7.43
CHEMBL502835 NINTEDANIB Kd = 73.0 nM 7.14
CHEMBL1908395 Kd = 120.0 nM 6.92
CHEMBL475251 R-406 Kd = 130.0 nM 6.89
CHEMBL601719 CRIZOTINIB Kd = 270.0 nM 6.57
CHEMBL288441 BOSUTINIB Kd = 360.0 nM 6.44
CHEMBL180022 NERATINIB Kd = 510.0 nM 6.29
CHEMBL574738 AST-487 Kd = 590.0 nM 6.23
CHEMBL535 SUNITINIB Kd = 1100.0 nM 5.96
CHEMBL1287853 FEDRATINIB Kd = 1100.0 nM 5.96
CHEMBL1908397 KW-2449 Kd = 1100.0 nM 5.96
CHEMBL608533 MIDOSTAURIN Kd = 1200.0 nM 5.92
CHEMBL477772 PAZOPANIB Kd = 2700.0 nM 5.57
CHEMBL386051 Kd = 3500.0 nM 5.46
CHEMBL572878 TOZASERTIB Kd = 4200.0 nM 5.38
CHEMBL259084 MLN-8054 Kd = 4400.0 nM 5.36
CHEMBL558752 RAF-265 Kd = 8600.0 nM 5.07
CHEMBL494089 GSK-690693 Kd > 10000.0 nM -
CHEMBL445813 AT-7519 Kd > 10000.0 nM -
CHEMBL31965 CANERTINIB Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL255863 NILOTINIB Kd > 10000.0 nM -
CHEMBL1336 SORAFENIB Kd > 10000.0 nM -
CHEMBL215152 DEFOSBARASERTIB Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -
CHEMBL491473 CEDIRANIB Kd > 10000.0 nM -
CHEMBL24828 VANDETANIB Kd > 10000.0 nM -
CHEMBL513909 BI-2536 Kd > 10000.0 nM -
CHEMBL5416410 DASATINIB Kd > 10000.0 nM -
CHEMBL1789941 RUXOLITINIB Kd > 10000.0 nM -
CHEMBL230011 TG100-115 Kd > 10000.0 nM -
CHEMBL1908394 GSK-461364 Kd > 10000.0 nM -
CHEMBL522892 DOVITINIB Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL521851 PICTILISIB Kd > 10000.0 nM -
CHEMBL377300 BRIVANIB Kd > 10000.0 nM -
CHEMBL939 GEFITINIB Kd > 10000.0 nM -
CHEMBL608154 Kd > 10000.0 nM -
CHEMBL10 SB-203580 Kd > 10000.0 nM -
CHEMBL1289926 AXITINIB Kd > 10000.0 nM -
CHEMBL221959 TOFACITINIB Kd > 10000.0 nM -
CHEMBL1614701 SELUMETINIB Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -
CHEMBL576982 QUIZARTINIB Kd > 10000.0 nM -
CHEMBL1236107 SGX-523 Kd > 10000.0 nM -