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Assay Detail

CHEMBL1908586

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Binding
Binding constant for JNK1 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

Mitogen-activated protein kinase 8 (CHEMBL2276)
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 6.04 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL603469 LESTAURTINIB 3.0 1 7.96
CHEMBL475251 R-406 2.0 1 7.42
CHEMBL509032 TAE-684 1 6.80
CHEMBL464552 1 6.68
CHEMBL388978 STAUROSPORINE 1 6.66
CHEMBL1287853 FEDRATINIB 4.0 1 6.58
CHEMBL255863 NILOTINIB 4.0 1 6.35
CHEMBL574738 AST-487 1.0 1 6.34
CHEMBL1908397 KW-2449 1.0 1 6.24
CHEMBL502835 NINTEDANIB 4.0 1 6.20
CHEMBL1908395 1 6.08
CHEMBL10 SB-203580 1 5.96
CHEMBL521851 PICTILISIB 2.0 1 5.82
CHEMBL386051 1 5.82
CHEMBL428690 ALVOCIDIB 3.0 1 5.80
CHEMBL477772 PAZOPANIB 4.0 1 5.70
CHEMBL180022 NERATINIB 4.0 1 5.48
CHEMBL1289926 AXITINIB 4.0 1 5.41
CHEMBL1236107 SGX-523 1.0 1 5.38
CHEMBL608533 MIDOSTAURIN 4.0 1 5.36
CHEMBL1789941 RUXOLITINIB 4.0 1 5.32
CHEMBL941 IMATINIB 4.0 1 5.30
CHEMBL1230609 FORETINIB 2.0 1 5.24
CHEMBL103667 DORAMAPIMOD 2.0 1 5.04
CHEMBL939 GEFITINIB 4.0 1 -
CHEMBL91829 RUBOXISTAURIN 3.0 1 -
CHEMBL215152 DEFOSBARASERTIB 2.0 1 -
CHEMBL384304 RG-547 2.0 1 -
CHEMBL261849 GW632580X 1 -
CHEMBL608154 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL603469 LESTAURTINIB Kd = 11.0 nM 7.96
CHEMBL475251 R-406 Kd = 38.0 nM 7.42
CHEMBL509032 TAE-684 Kd = 160.0 nM 6.80
CHEMBL464552 Kd = 210.0 nM 6.68
CHEMBL388978 STAUROSPORINE Kd = 220.0 nM 6.66
CHEMBL1287853 FEDRATINIB Kd = 260.0 nM 6.58
CHEMBL255863 NILOTINIB Kd = 450.0 nM 6.35
CHEMBL574738 AST-487 Kd = 460.0 nM 6.34
CHEMBL1908397 KW-2449 Kd = 580.0 nM 6.24
CHEMBL502835 NINTEDANIB Kd = 630.0 nM 6.20
CHEMBL1908395 Kd = 830.0 nM 6.08
CHEMBL10 SB-203580 Kd = 1100.0 nM 5.96
CHEMBL521851 PICTILISIB Kd = 1500.0 nM 5.82
CHEMBL386051 Kd = 1500.0 nM 5.82
CHEMBL428690 ALVOCIDIB Kd = 1600.0 nM 5.80
CHEMBL477772 PAZOPANIB Kd = 2000.0 nM 5.70
CHEMBL180022 NERATINIB Kd = 3300.0 nM 5.48
CHEMBL1289926 AXITINIB Kd = 3900.0 nM 5.41
CHEMBL1236107 SGX-523 Kd = 4200.0 nM 5.38
CHEMBL608533 MIDOSTAURIN Kd = 4400.0 nM 5.36
CHEMBL1789941 RUXOLITINIB Kd = 4800.0 nM 5.32
CHEMBL941 IMATINIB Kd = 5000.0 nM 5.30
CHEMBL1230609 FORETINIB Kd = 5700.0 nM 5.24
CHEMBL103667 DORAMAPIMOD Kd = 9100.0 nM 5.04
CHEMBL288441 BOSUTINIB Kd > 10000.0 nM -
CHEMBL300138 ENZASTAURIN Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL494089 GSK-690693 Kd > 10000.0 nM -
CHEMBL1336 SORAFENIB Kd > 10000.0 nM -
CHEMBL1241674 Kd > 10000.0 nM -
CHEMBL221959 TOFACITINIB Kd > 10000.0 nM -
CHEMBL1721885 SU-014813 Kd > 10000.0 nM -
CHEMBL1614701 SELUMETINIB Kd > 10000.0 nM -
CHEMBL601719 CRIZOTINIB Kd > 10000.0 nM -
CHEMBL450786 PHA-665752 Kd > 10000.0 nM -
CHEMBL535 SUNITINIB Kd > 10000.0 nM -
CHEMBL445813 AT-7519 Kd > 10000.0 nM -
CHEMBL259084 MLN-8054 Kd > 10000.0 nM -
CHEMBL1908394 GSK-461364 Kd > 10000.0 nM -
CHEMBL522892 DOVITINIB Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL31965 CANERTINIB Kd > 10000.0 nM -
CHEMBL608154 Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL384304 RG-547 Kd > 10000.0 nM -
CHEMBL215152 DEFOSBARASERTIB Kd > 10000.0 nM -
CHEMBL91829 RUBOXISTAURIN Kd > 10000.0 nM -
CHEMBL939 GEFITINIB Kd > 10000.0 nM -