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Assay Detail

CHEMBL1908613

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Binding
Binding constant for ULK1 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

Serine/threonine-protein kinase ULK1 (CHEMBL6006)
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 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL509032 TAE-684 1 9.08
CHEMBL388978 STAUROSPORINE 1 8.00
CHEMBL475251 R-406 2.0 1 7.85
CHEMBL535 SUNITINIB 4.0 1 7.64
CHEMBL1908397 KW-2449 1.0 1 7.28
CHEMBL522892 DOVITINIB 3.0 1 7.26
CHEMBL1721885 SU-014813 2.0 1 7.09
CHEMBL1287853 FEDRATINIB 4.0 1 6.57
CHEMBL1789941 RUXOLITINIB 4.0 1 6.52
CHEMBL502835 NINTEDANIB 4.0 1 6.47
CHEMBL603469 LESTAURTINIB 3.0 1 6.00
CHEMBL601719 CRIZOTINIB 4.0 1 6.00
CHEMBL288441 BOSUTINIB 4.0 1 5.92
CHEMBL1908395 1 5.72
CHEMBL450786 PHA-665752 1 5.70
CHEMBL296468 BMS-387032 1.0 1 5.55
CHEMBL574738 AST-487 1.0 1 5.43
CHEMBL494089 GSK-690693 1.0 1 5.23
CHEMBL379218 1 5.10
CHEMBL124660 TANDUTINIB 2.0 1 -
CHEMBL259084 MLN-8054 1.0 1 -
CHEMBL464552 1 -
CHEMBL10 SB-203580 1 -
CHEMBL608154 1 -
CHEMBL939 GEFITINIB 4.0 1 -
CHEMBL1289926 AXITINIB 4.0 1 -
CHEMBL384304 RG-547 2.0 1 -
CHEMBL180022 NERATINIB 4.0 1 -
CHEMBL91829 RUBOXISTAURIN 3.0 1 -
CHEMBL377300 BRIVANIB 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL509032 TAE-684 Kd = 0.83 nM 9.08
CHEMBL388978 STAUROSPORINE Kd = 9.9 nM 8.00
CHEMBL475251 R-406 Kd = 14.0 nM 7.85
CHEMBL535 SUNITINIB Kd = 23.0 nM 7.64
CHEMBL1908397 KW-2449 Kd = 53.0 nM 7.28
CHEMBL522892 DOVITINIB Kd = 55.0 nM 7.26
CHEMBL1721885 SU-014813 Kd = 82.0 nM 7.09
CHEMBL1287853 FEDRATINIB Kd = 270.0 nM 6.57
CHEMBL1789941 RUXOLITINIB Kd = 300.0 nM 6.52
CHEMBL502835 NINTEDANIB Kd = 340.0 nM 6.47
CHEMBL603469 LESTAURTINIB Kd = 1000.0 nM 6.00
CHEMBL601719 CRIZOTINIB Kd = 1000.0 nM 6.00
CHEMBL288441 BOSUTINIB Kd = 1200.0 nM 5.92
CHEMBL1908395 Kd = 1900.0 nM 5.72
CHEMBL450786 PHA-665752 Kd = 2000.0 nM 5.70
CHEMBL296468 BMS-387032 Kd = 2800.0 nM 5.55
CHEMBL574738 AST-487 Kd = 3700.0 nM 5.43
CHEMBL494089 GSK-690693 Kd = 5900.0 nM 5.23
CHEMBL379218 Kd = 8000.0 nM 5.10
CHEMBL573339 PI-103 Kd > 10000.0 nM -
CHEMBL513909 BI-2536 Kd > 10000.0 nM -
CHEMBL941 IMATINIB Kd > 10000.0 nM -
CHEMBL1614701 SELUMETINIB Kd > 10000.0 nM -
CHEMBL386051 Kd > 10000.0 nM -
CHEMBL221959 TOFACITINIB Kd > 10000.0 nM -
CHEMBL1241674 Kd > 10000.0 nM -
CHEMBL477772 PAZOPANIB Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL215152 DEFOSBARASERTIB Kd > 10000.0 nM -
CHEMBL31965 CANERTINIB Kd > 10000.0 nM -
CHEMBL445813 AT-7519 Kd > 10000.0 nM -
CHEMBL1336 SORAFENIB Kd > 10000.0 nM -
CHEMBL255863 NILOTINIB Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL572878 TOZASERTIB Kd > 10000.0 nM -
CHEMBL1908394 GSK-461364 Kd > 10000.0 nM -
CHEMBL105442 CI-1040 Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL1236107 SGX-523 Kd > 10000.0 nM -
CHEMBL377300 BRIVANIB Kd > 10000.0 nM -
CHEMBL91829 RUBOXISTAURIN Kd > 10000.0 nM -
CHEMBL180022 NERATINIB Kd > 10000.0 nM -
CHEMBL384304 RG-547 Kd > 10000.0 nM -
CHEMBL1289926 AXITINIB Kd > 10000.0 nM -
CHEMBL939 GEFITINIB Kd > 10000.0 nM -
CHEMBL608154 Kd > 10000.0 nM -
CHEMBL10 SB-203580 Kd > 10000.0 nM -
CHEMBL464552 Kd > 10000.0 nM -
CHEMBL259084 MLN-8054 Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -