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Assay Detail

CHEMBL2175553

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

Binding
Inhibition of PI3Kalpha by AlphaScreen assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Publication

Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Peterson EA, Boezio AA, Andrews PS, Boezio CM, Bush TL, Cheng AC, Choquette D, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Kim JL, Lewis RT, Liu J, Mullady EL, Potashman MH, Romero K, Shaffer PL, Stanton MK, Stellwagen JC, Teffera Y, Yi S, Cai T, La DS.
Bioorg Med Chem Lett (2012) 22 : 4967 -4974
PubMed 22765895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.43 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172629 1 7.33
CHEMBL2172635 1 7.27
CHEMBL2172486 1 7.17
CHEMBL2172482 1 7.14
CHEMBL2172485 1 7.07
CHEMBL2172487 1 7.02
CHEMBL2172634 1 6.98
CHEMBL2172475 1 6.95
CHEMBL2172636 1 6.92
CHEMBL2172480 1 6.92
CHEMBL2172630 1 6.91
CHEMBL2172489 1 6.84
CHEMBL2172632 1 6.76
CHEMBL2172490 1 6.75
CHEMBL2172484 1 6.62
CHEMBL2172633 1 6.59
CHEMBL2172483 1 6.57
CHEMBL2172640 1 6.51
CHEMBL2172481 1 6.41
CHEMBL2172488 1 6.33
CHEMBL2172637 1 6.23
CHEMBL2172624 1 6.20
CHEMBL2172638 1 6.19
CHEMBL2172639 1 6.18
CHEMBL2172625 1 6.12
CHEMBL1615183 1 6.10
CHEMBL2172627 1 5.94
CHEMBL2172631 1 5.94
CHEMBL2172474 1 5.78
CHEMBL2172628 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172629 IC50 = 47.0 nM 7.33
CHEMBL2172635 IC50 = 54.0 nM 7.27
CHEMBL2172486 IC50 = 68.0 nM 7.17
CHEMBL2172482 IC50 = 73.0 nM 7.14
CHEMBL2172485 IC50 = 85.0 nM 7.07
CHEMBL2172487 IC50 = 96.0 nM 7.02
CHEMBL2172634 IC50 = 105.0 nM 6.98
CHEMBL2172475 IC50 = 112.0 nM 6.95
CHEMBL2172636 IC50 = 119.0 nM 6.92
CHEMBL2172480 IC50 = 120.0 nM 6.92
CHEMBL2172630 IC50 = 122.0 nM 6.91
CHEMBL2172489 IC50 = 144.0 nM 6.84
CHEMBL2172632 IC50 = 173.0 nM 6.76
CHEMBL2172490 IC50 = 177.0 nM 6.75
CHEMBL2172484 IC50 = 239.0 nM 6.62
CHEMBL2172633 IC50 = 256.0 nM 6.59
CHEMBL2172483 IC50 = 268.0 nM 6.57
CHEMBL2172640 IC50 = 306.0 nM 6.51
CHEMBL2172481 IC50 = 393.0 nM 6.41
CHEMBL2172488 IC50 = 463.0 nM 6.33
CHEMBL2172637 IC50 = 590.0 nM 6.23
CHEMBL2172624 IC50 = 635.0 nM 6.20
CHEMBL2172638 IC50 = 648.0 nM 6.19
CHEMBL2172639 IC50 = 654.0 nM 6.18
CHEMBL2172625 IC50 = 763.0 nM 6.12
CHEMBL1615183 IC50 = 798.0 nM 6.10
CHEMBL2172627 IC50 = 1140.0 nM 5.94
CHEMBL2172631 IC50 = 1140.0 nM 5.94
CHEMBL2172474 IC50 = 1660.0 nM 5.78
CHEMBL2172628 IC50 = 3020.0 nM 5.52
CHEMBL2172479 IC50 = 3170.0 nM 5.50
CHEMBL2172477 IC50 = 4290.0 nM 5.37
CHEMBL2172476 IC50 = 4580.0 nM 5.34
CHEMBL2172626 IC50 = 5840.0 nM 5.23
CHEMBL2172478 IC50 > 125000.0 nM -