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Assay Detail

CHEMBL1908413

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Binding
Binding constant for CSNK1D 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

Casein kinase I isoform delta (CHEMBL2828)
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 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535 SUNITINIB 4.0 1 7.82
CHEMBL10 SB-203580 1 7.43
CHEMBL379218 1 6.68
CHEMBL288441 BOSUTINIB 4.0 1 6.62
CHEMBL1721885 SU-014813 2.0 1 6.58
CHEMBL1241674 1 6.50
CHEMBL521851 PICTILISIB 2.0 1 5.92
CHEMBL230011 TG100-115 2.0 1 5.89
CHEMBL502835 NINTEDANIB 4.0 1 5.89
CHEMBL525191 1 5.85
CHEMBL513909 BI-2536 2.0 1 5.82
CHEMBL296468 BMS-387032 1.0 1 5.75
CHEMBL1908397 KW-2449 1.0 1 5.64
CHEMBL388978 STAUROSPORINE 1 5.62
CHEMBL574738 AST-487 1.0 1 5.60
CHEMBL939 GEFITINIB 4.0 1 5.50
CHEMBL553 ERLOTINIB 4.0 1 5.46
CHEMBL464552 1 5.46
CHEMBL450786 PHA-665752 1 5.38
CHEMBL31965 CANERTINIB 3.0 1 5.34
CHEMBL384304 RG-547 2.0 1 -
CHEMBL1289926 AXITINIB 4.0 1 -
CHEMBL608154 1 -
CHEMBL377300 BRIVANIB 3.0 1 -
CHEMBL576982 QUIZARTINIB 4.0 1 -
CHEMBL1336 SORAFENIB 4.0 1 -
CHEMBL91829 RUBOXISTAURIN 3.0 1 -
CHEMBL261849 GW632580X 1 -
CHEMBL477772 PAZOPANIB 4.0 1 -
CHEMBL1908391 MASITINIB 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535 SUNITINIB Kd = 15.0 nM 7.82
CHEMBL10 SB-203580 Kd = 37.0 nM 7.43
CHEMBL379218 Kd = 210.0 nM 6.68
CHEMBL288441 BOSUTINIB Kd = 240.0 nM 6.62
CHEMBL1721885 SU-014813 Kd = 260.0 nM 6.58
CHEMBL1241674 Kd = 320.0 nM 6.50
CHEMBL521851 PICTILISIB Kd = 1200.0 nM 5.92
CHEMBL230011 TG100-115 Kd = 1300.0 nM 5.89
CHEMBL502835 NINTEDANIB Kd = 1300.0 nM 5.89
CHEMBL525191 Kd = 1400.0 nM 5.85
CHEMBL513909 BI-2536 Kd = 1500.0 nM 5.82
CHEMBL296468 BMS-387032 Kd = 1800.0 nM 5.75
CHEMBL1908397 KW-2449 Kd = 2300.0 nM 5.64
CHEMBL388978 STAUROSPORINE Kd = 2400.0 nM 5.62
CHEMBL574738 AST-487 Kd = 2500.0 nM 5.60
CHEMBL939 GEFITINIB Kd = 3200.0 nM 5.50
CHEMBL464552 Kd = 3500.0 nM 5.46
CHEMBL553 ERLOTINIB Kd = 3500.0 nM 5.46
CHEMBL450786 PHA-665752 Kd = 4200.0 nM 5.38
CHEMBL31965 CANERTINIB Kd = 4600.0 nM 5.34
CHEMBL522892 DOVITINIB Kd > 10000.0 nM -
CHEMBL1614701 SELUMETINIB Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -
CHEMBL494089 GSK-690693 Kd > 10000.0 nM -
CHEMBL1236107 SGX-523 Kd > 10000.0 nM -
CHEMBL445813 AT-7519 Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL1908394 GSK-461364 Kd > 10000.0 nM -
CHEMBL1173655 AFATINIB Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -
CHEMBL180022 NERATINIB Kd > 10000.0 nM -
CHEMBL386051 Kd > 10000.0 nM -
CHEMBL491473 CEDIRANIB Kd > 10000.0 nM -
CHEMBL221959 TOFACITINIB Kd > 10000.0 nM -
CHEMBL941 IMATINIB Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL255863 NILOTINIB Kd > 10000.0 nM -
CHEMBL259084 MLN-8054 Kd > 10000.0 nM -
CHEMBL603469 LESTAURTINIB Kd > 10000.0 nM -
CHEMBL223360 LINIFANIB Kd > 10000.0 nM -
CHEMBL1908391 MASITINIB Kd > 10000.0 nM -
CHEMBL477772 PAZOPANIB Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL91829 RUBOXISTAURIN Kd > 10000.0 nM -
CHEMBL1336 SORAFENIB Kd > 10000.0 nM -
CHEMBL576982 QUIZARTINIB Kd > 10000.0 nM -
CHEMBL377300 BRIVANIB Kd > 10000.0 nM -
CHEMBL608154 Kd > 10000.0 nM -
CHEMBL1289926 AXITINIB Kd > 10000.0 nM -
CHEMBL384304 RG-547 Kd > 10000.0 nM -