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Assay Detail

CHEMBL1908588

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Binding
Binding constant for JNK3 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 10 (CHEMBL2637)
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 6.09 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL603469 LESTAURTINIB 3.0 1 7.92
CHEMBL10 SB-203580 1 7.46
CHEMBL475251 R-406 2.0 1 7.43
CHEMBL1908397 KW-2449 1.0 1 7.29
CHEMBL509032 TAE-684 1 7.17
CHEMBL388978 STAUROSPORINE 1 6.96
CHEMBL103667 DORAMAPIMOD 2.0 1 6.96
CHEMBL464552 1 6.89
CHEMBL1287853 FEDRATINIB 4.0 1 6.70
CHEMBL1908395 1 6.62
CHEMBL502835 NINTEDANIB 4.0 1 6.57
CHEMBL521851 PICTILISIB 2.0 1 6.25
CHEMBL574738 AST-487 1.0 1 6.12
CHEMBL513909 BI-2536 2.0 1 5.96
CHEMBL1289926 AXITINIB 4.0 1 5.96
CHEMBL477772 PAZOPANIB 4.0 1 5.72
CHEMBL1236107 SGX-523 1.0 1 5.72
CHEMBL255863 NILOTINIB 4.0 1 5.70
CHEMBL1173655 AFATINIB 4.0 1 5.70
CHEMBL180022 NERATINIB 4.0 1 5.60
CHEMBL525191 1 5.60
CHEMBL572878 TOZASERTIB 2.0 1 5.55
CHEMBL941 IMATINIB 4.0 1 5.51
CHEMBL939 GEFITINIB 4.0 1 5.50
CHEMBL608533 MIDOSTAURIN 4.0 1 5.44
CHEMBL1721885 SU-014813 2.0 1 5.44
CHEMBL1230609 FORETINIB 2.0 1 5.41
CHEMBL223360 LINIFANIB 3.0 1 5.37
CHEMBL535 SUNITINIB 4.0 1 5.37
CHEMBL553 ERLOTINIB 4.0 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL603469 LESTAURTINIB Kd = 12.0 nM 7.92
CHEMBL10 SB-203580 Kd = 35.0 nM 7.46
CHEMBL475251 R-406 Kd = 37.0 nM 7.43
CHEMBL1908397 KW-2449 Kd = 51.0 nM 7.29
CHEMBL509032 TAE-684 Kd = 67.0 nM 7.17
CHEMBL388978 STAUROSPORINE Kd = 110.0 nM 6.96
CHEMBL103667 DORAMAPIMOD Kd = 110.0 nM 6.96
CHEMBL464552 Kd = 130.0 nM 6.89
CHEMBL1287853 FEDRATINIB Kd = 200.0 nM 6.70
CHEMBL1908395 Kd = 240.0 nM 6.62
CHEMBL502835 NINTEDANIB Kd = 270.0 nM 6.57
CHEMBL521851 PICTILISIB Kd = 560.0 nM 6.25
CHEMBL574738 AST-487 Kd = 760.0 nM 6.12
CHEMBL513909 BI-2536 Kd = 1100.0 nM 5.96
CHEMBL1289926 AXITINIB Kd = 1100.0 nM 5.96
CHEMBL477772 PAZOPANIB Kd = 1900.0 nM 5.72
CHEMBL1236107 SGX-523 Kd = 1900.0 nM 5.72
CHEMBL255863 NILOTINIB Kd = 2000.0 nM 5.70
CHEMBL1173655 AFATINIB Kd = 2000.0 nM 5.70
CHEMBL180022 NERATINIB Kd = 2500.0 nM 5.60
CHEMBL525191 Kd = 2500.0 nM 5.60
CHEMBL572878 TOZASERTIB Kd = 2800.0 nM 5.55
CHEMBL941 IMATINIB Kd = 3100.0 nM 5.51
CHEMBL939 GEFITINIB Kd = 3200.0 nM 5.50
CHEMBL1721885 SU-014813 Kd = 3600.0 nM 5.44
CHEMBL608533 MIDOSTAURIN Kd = 3600.0 nM 5.44
CHEMBL1230609 FORETINIB Kd = 3900.0 nM 5.41
CHEMBL223360 LINIFANIB Kd = 4300.0 nM 5.37
CHEMBL535 SUNITINIB Kd = 4300.0 nM 5.37
CHEMBL553 ERLOTINIB Kd = 4300.0 nM 5.37
CHEMBL428690 ALVOCIDIB Kd = 5500.0 nM 5.26
CHEMBL31965 CANERTINIB Kd = 5500.0 nM 5.26
CHEMBL296468 BMS-387032 Kd = 5900.0 nM 5.23
CHEMBL221959 TOFACITINIB Kd > 10000.0 nM -
CHEMBL1241674 Kd > 10000.0 nM -
CHEMBL259084 MLN-8054 Kd > 10000.0 nM -
CHEMBL1908394 GSK-461364 Kd > 10000.0 nM -
CHEMBL288441 BOSUTINIB Kd > 10000.0 nM -
CHEMBL522892 DOVITINIB Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -
CHEMBL494089 GSK-690693 Kd > 10000.0 nM -
CHEMBL1336 SORAFENIB Kd > 10000.0 nM -
CHEMBL445813 AT-7519 Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL215152 DEFOSBARASERTIB Kd > 10000.0 nM -
CHEMBL608154 Kd > 10000.0 nM -
CHEMBL300138 ENZASTAURIN Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -