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Assay Detail

CHEMBL3587362

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of PI3K-alpha (unknown origin) by mobility shift assay
30
Total Activities
30
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

Publication

Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Zhao J, Packard G, Bahmanyar S, Correa M, Elsner J, Harris R, Lee BG, Papa P, Parnes JS, Riggs JR, Sapienza J, Tehrani L, Whitefield B, Apuy J, Bisonette RR, Gamez JC, Hickman M, Khambatta G, Leisten J, Peng SX, Richardson SJ, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S.
J Med Chem (2015) 58 : 5323 -5333
PubMed 26083478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.59 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3586382 1 7.00
CHEMBL3586384 1 6.92
CHEMBL3586383 1 6.70
CHEMBL3586387 1 6.29
CHEMBL2348864 1 6.28
CHEMBL3586385 1 5.80
CHEMBL3586401 1 5.72
CHEMBL3586386 1 5.64
CHEMBL3586397 1 5.60
CHEMBL3586400 1 5.55
CHEMBL3586393 1 5.50
CHEMBL3586394 1 5.42
CHEMBL3586404 ONATASERTIB 2.0 1 5.40
CHEMBL3586392 1 5.33
CHEMBL3586399 1 5.33
CHEMBL3586391 1 5.21
CHEMBL3586396 1 5.12
CHEMBL3586390 1 4.98
CHEMBL3586402 1 4.96
CHEMBL3586403 1 4.79
CHEMBL3586395 1 4.75
CHEMBL3586398 1 4.70
CHEMBL3585359 1 -
CHEMBL3586388 1 -
CHEMBL3586379 1 -
CHEMBL3586380 1 -
CHEMBL3586381 1 -
CHEMBL3586389 1 -
CHEMBL2348862 1 -
CHEMBL3586405 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3586382 IC50 = 100.0 nM 7.00
CHEMBL3586384 IC50 = 120.0 nM 6.92
CHEMBL3586383 IC50 = 200.0 nM 6.70
CHEMBL3586387 IC50 = 510.0 nM 6.29
CHEMBL2348864 IC50 = 530.0 nM 6.28
CHEMBL3586385 IC50 = 1600.0 nM 5.80
CHEMBL3586401 IC50 = 1900.0 nM 5.72
CHEMBL3586386 IC50 = 2300.0 nM 5.64
CHEMBL3586397 IC50 = 2500.0 nM 5.60
CHEMBL3586400 IC50 = 2800.0 nM 5.55
CHEMBL3586393 IC50 = 3200.0 nM 5.50
CHEMBL3586394 IC50 = 3800.0 nM 5.42
CHEMBL3586404 ONATASERTIB IC50 = 4000.0 nM 5.40
CHEMBL3586392 IC50 = 4700.0 nM 5.33
CHEMBL3586399 IC50 = 4700.0 nM 5.33
CHEMBL3586391 IC50 = 6200.0 nM 5.21
CHEMBL3586396 IC50 = 7600.0 nM 5.12
CHEMBL3586390 IC50 = 10500.0 nM 4.98
CHEMBL3586402 IC50 = 11100.0 nM 4.96
CHEMBL3586403 IC50 = 16400.0 nM 4.79
CHEMBL3586395 IC50 = 17700.0 nM 4.75
CHEMBL3586398 IC50 = 20200.0 nM 4.70
CHEMBL3585359 IC50 - -
CHEMBL3586388 IC50 - -
CHEMBL3586379 IC50 - -
CHEMBL3586380 IC50 - -
CHEMBL3586381 IC50 - -
CHEMBL3586389 IC50 - -
CHEMBL2348862 IC50 > 30000.0 nM -
CHEMBL3586405 IC50 > 30000.0 nM -