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Assay Detail

CHEMBL3824711

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Binding
Inhibition of human InsR using myelin basic protein as substrate and [gamma-33P]ATP measured after 1 hr
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Insulin receptor (CHEMBL1981) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Huang WS, Liu S, Zou D, Thomas M, Wang Y, Zhou T, Romero J, Kohlmann A, Li F, Qi J, Cai L, Dwight TA, Xu Y, Xu R, Dodd R, Toms A, Parillon L, Lu X, Anjum R, Zhang S, Wang F, Keats J, Wardwell SD, Ning Y, Xu Q, Moran LE, Mohemmad QK, Jang HG, Clackson T, Narasimhan NI, Rivera VM, Zhu X, Dalgarno D, Shakespeare WC.
J Med Chem (2016) 59 : 4948 -4964
PubMed 27144831 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 7.03 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3824326 — — 1 9.06
CHEMBL509032 TAE-684 — 1 8.72
CHEMBL3824301 — — 1 8.67
CHEMBL3824246 — — 1 8.47
CHEMBL3823256 — — 1 8.33
CHEMBL3822475 — — 1 8.29
CHEMBL3823016 — — 1 8.22
CHEMBL3822672 — — 1 8.07
CHEMBL3824304 — — 1 8.00
CHEMBL3822664 — — 1 7.86
CHEMBL3823268 — — 1 7.85
CHEMBL3823045 — — 1 7.58
CHEMBL3823235 — — 1 7.55
CHEMBL3822499 — — 1 7.37
CHEMBL3822982 — — 1 7.26
CHEMBL3823190 — — 1 7.24
CHEMBL3824185 — — 1 7.09
CHEMBL3823031 — — 1 7.07
CHEMBL3822611 — — 1 7.04
CHEMBL3397300 — — 1 7.00
CHEMBL3824007 — — 1 6.99
CHEMBL3823218 — — 1 6.89
CHEMBL3823864 — — 1 6.89
CHEMBL3824290 — — 1 6.79
CHEMBL3823017 — — 1 6.77
CHEMBL3823836 — — 1 6.77
CHEMBL3545311 BRIGATINIB 4.0 1 6.71
CHEMBL601719 CRIZOTINIB 4.0 1 6.70
CHEMBL3824318 — — 1 6.60
CHEMBL3822557 — — 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3824326 — IC50 = 0.88 nM 9.06
CHEMBL509032 TAE-684 IC50 = 1.9 nM 8.72
CHEMBL3824301 — IC50 = 2.16 nM 8.67
CHEMBL3824246 — IC50 = 3.4 nM 8.47
CHEMBL3823256 — IC50 = 4.7 nM 8.33
CHEMBL3822475 — IC50 = 5.1 nM 8.29
CHEMBL3823016 — IC50 = 6.05 nM 8.22
CHEMBL3822672 — IC50 = 8.44 nM 8.07
CHEMBL3824304 — IC50 = 9.9 nM 8.00
CHEMBL3822664 — IC50 = 13.7 nM 7.86
CHEMBL3823268 — IC50 = 14.1 nM 7.85
CHEMBL3823045 — IC50 = 26.0 nM 7.58
CHEMBL3823235 — IC50 = 28.1 nM 7.55
CHEMBL3822499 — IC50 = 43.2 nM 7.37
CHEMBL3822982 — IC50 = 55.2 nM 7.26
CHEMBL3823190 — IC50 = 57.2 nM 7.24
CHEMBL3824185 — IC50 = 81.7 nM 7.09
CHEMBL3823031 — IC50 = 85.3 nM 7.07
CHEMBL3822611 — IC50 = 90.6 nM 7.04
CHEMBL3397300 — IC50 = 100.0 nM 7.00
CHEMBL3824007 — IC50 = 103.0 nM 6.99
CHEMBL3823218 — IC50 = 130.0 nM 6.89
CHEMBL3823864 — IC50 = 128.0 nM 6.89
CHEMBL3824290 — IC50 = 162.0 nM 6.79
CHEMBL3823836 — IC50 = 171.0 nM 6.77
CHEMBL3823017 — IC50 = 171.0 nM 6.77
CHEMBL3545311 BRIGATINIB IC50 = 196.0 nM 6.71
CHEMBL601719 CRIZOTINIB IC50 = 201.0 nM 6.70
CHEMBL3824318 — IC50 = 253.0 nM 6.60
CHEMBL3822557 — IC50 = 270.0 nM 6.57
CHEMBL3823243 — IC50 = 270.0 nM 6.57
CHEMBL3823549 — IC50 = 284.0 nM 6.55
CHEMBL3824327 — IC50 = 285.0 nM 6.54
CHEMBL3824308 — IC50 = 314.0 nM 6.50
CHEMBL3824130 — IC50 = 339.0 nM 6.47
CHEMBL3823916 — IC50 = 343.0 nM 6.46
CHEMBL3822524 — IC50 = 367.0 nM 6.43
CHEMBL3823603 — IC50 = 397.0 nM 6.40
CHEMBL3823416 — IC50 = 399.0 nM 6.40
CHEMBL3823872 — IC50 = 459.0 nM 6.34
CHEMBL3823577 — IC50 = 483.0 nM 6.32
CHEMBL3823107 — IC50 = 489.0 nM 6.31
CHEMBL3823224 — IC50 = 700.0 nM 6.16
CHEMBL3822645 — IC50 = 702.0 nM 6.15
CHEMBL3823165 — IC50 = 726.0 nM 6.14
CHEMBL3823078 — IC50 = 1179.0 nM 5.93
CHEMBL3823296 — IC50 = 1683.0 nM 5.77
CHEMBL3823198 — IC50 = 1684.0 nM 5.77
CHEMBL3822973 — IC50 - — -
CHEMBL3822589 — IC50 - — -