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Assay Detail

CHEMBL1243965

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

Binding
Inhibition of recombinant PI3Kalpha by radioactive phosphotransfer assay in presence of 10 uM ATP
209
Total Activities
209
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA.
Nat Chem Biol (2008) 4 : 691 -699
PubMed 18849971 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 209 5.72 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1233881 1 7.77
CHEMBL1233882 1 7.77
CHEMBL1242756 1 7.46
CHEMBL1241578 1 7.34
CHEMBL1081312 1 7.28
CHEMBL1242201 1 7.17
CHEMBL1241299 1 7.16
CHEMBL1241681 1 7.16
CHEMBL1242477 1 7.16
CHEMBL1242287 1 7.12
CHEMBL1242290 1 7.10
CHEMBL1241776 1 7.10
CHEMBL1242572 1 7.09
CHEMBL1241944 1 7.07
CHEMBL1240565 1 7.04
CHEMBL1241945 1 7.04
CHEMBL1241678 1 6.95
CHEMBL1242293 1 6.92
CHEMBL1241484 1 6.87
CHEMBL1240554 1 6.87
CHEMBL1242376 1 6.85
CHEMBL1242386 1 6.84
CHEMBL1242573 1 6.84
CHEMBL1242114 1 6.79
CHEMBL1242198 1 6.76
CHEMBL1241580 1 6.75
CHEMBL1242377 1 6.73
CHEMBL1242202 1 6.72
CHEMBL1242476 1 6.71
CHEMBL1241774 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1233882 IC50 = 17.0 nM 7.77
CHEMBL1233881 IC50 = 17.0 nM 7.77
CHEMBL1242756 IC50 = 35.0 nM 7.46
CHEMBL1241578 IC50 = 46.0 nM 7.34
CHEMBL1081312 IC50 = 52.0 nM 7.28
CHEMBL1242201 IC50 = 68.0 nM 7.17
CHEMBL1241299 IC50 = 70.0 nM 7.16
CHEMBL1242477 IC50 = 69.0 nM 7.16
CHEMBL1241681 IC50 = 70.0 nM 7.16
CHEMBL1242287 IC50 = 76.0 nM 7.12
CHEMBL1242290 IC50 = 80.0 nM 7.10
CHEMBL1241776 IC50 = 80.0 nM 7.10
CHEMBL1242572 IC50 = 82.0 nM 7.09
CHEMBL1241944 IC50 = 86.0 nM 7.07
CHEMBL1241945 IC50 = 92.0 nM 7.04
CHEMBL1240565 IC50 = 91.0 nM 7.04
CHEMBL1241678 IC50 = 113.0 nM 6.95
CHEMBL1242293 IC50 = 120.0 nM 6.92
CHEMBL1240554 IC50 = 135.0 nM 6.87
CHEMBL1241484 IC50 = 135.0 nM 6.87
CHEMBL1242376 IC50 = 142.0 nM 6.85
CHEMBL1242386 IC50 = 145.0 nM 6.84
CHEMBL1242573 IC50 = 144.0 nM 6.84
CHEMBL1242114 IC50 = 164.0 nM 6.79
CHEMBL1242198 IC50 = 175.0 nM 6.76
CHEMBL1241580 IC50 = 176.0 nM 6.75
CHEMBL1242377 IC50 = 187.0 nM 6.73
CHEMBL1242202 IC50 = 192.0 nM 6.72
CHEMBL1242476 IC50 = 193.0 nM 6.71
CHEMBL1241774 IC50 = 206.0 nM 6.69
CHEMBL1242475 IC50 = 209.0 nM 6.68
CHEMBL1241676 IC50 = 225.0 nM 6.65
CHEMBL1242750 IC50 = 244.0 nM 6.61
CHEMBL1241949 IC50 = 245.0 nM 6.61
CHEMBL1242112 IC50 = 260.0 nM 6.58
CHEMBL1242199 IC50 = 266.0 nM 6.58
CHEMBL1242113 IC50 = 276.0 nM 6.56
CHEMBL1242026 IC50 = 280.0 nM 6.55
CHEMBL1240553 IC50 = 289.0 nM 6.54
CHEMBL1242028 IC50 = 296.0 nM 6.53
CHEMBL1241768 IC50 = 293.0 nM 6.53
CHEMBL1242119 IC50 = 344.0 nM 6.46
CHEMBL1242656 IC50 = 347.0 nM 6.46
CHEMBL1242470 IC50 = 394.0 nM 6.41
CHEMBL1241301 IC50 = 403.0 nM 6.39
CHEMBL1242752 IC50 = 433.0 nM 6.36
CHEMBL1242666 IC50 = 450.0 nM 6.35
CHEMBL1242208 IC50 = 443.0 nM 6.35
CHEMBL1241682 IC50 = 462.0 nM 6.33
CHEMBL1242379 IC50 = 464.0 nM 6.33