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Assay Detail

CHEMBL1243968

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

Binding
Inhibition of recombinant PI3Kgamma 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 5.81 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1241944 1 7.55
CHEMBL1241299 1 7.41
CHEMBL1233882 1 7.37
CHEMBL1241768 1 7.37
CHEMBL1242287 1 7.36
CHEMBL1242376 1 7.27
CHEMBL1241678 1 7.24
CHEMBL1242119 1 7.22
CHEMBL1233881 1 7.14
CHEMBL1240544 1 7.10
CHEMBL1240553 1 7.06
CHEMBL1241776 1 7.05
CHEMBL1242475 1 7.05
CHEMBL1241774 1 7.02
CHEMBL1242476 1 7.00
CHEMBL1241578 1 7.00
CHEMBL1242202 1 6.95
CHEMBL1242386 1 6.95
CHEMBL1240554 1 6.94
CHEMBL1242028 1 6.93
CHEMBL1242201 1 6.92
CHEMBL1242294 1 6.91
CHEMBL1241484 1 6.85
CHEMBL1242666 1 6.85
CHEMBL1241676 1 6.83
CHEMBL1242208 1 6.78
CHEMBL1241683 1 6.74
CHEMBL1241945 1 6.73
CHEMBL1242112 1 6.72
CHEMBL1241767 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1241944 IC50 = 28.0 nM 7.55
CHEMBL1241299 IC50 = 39.0 nM 7.41
CHEMBL1233882 IC50 = 43.0 nM 7.37
CHEMBL1241768 IC50 = 43.0 nM 7.37
CHEMBL1242287 IC50 = 44.0 nM 7.36
CHEMBL1242376 IC50 = 54.0 nM 7.27
CHEMBL1241678 IC50 = 58.0 nM 7.24
CHEMBL1242119 IC50 = 60.0 nM 7.22
CHEMBL1233881 IC50 = 72.0 nM 7.14
CHEMBL1240544 IC50 = 80.0 nM 7.10
CHEMBL1240553 IC50 = 87.0 nM 7.06
CHEMBL1241776 IC50 = 89.0 nM 7.05
CHEMBL1242475 IC50 = 90.0 nM 7.05
CHEMBL1241774 IC50 = 95.0 nM 7.02
CHEMBL1242476 IC50 = 101.0 nM 7.00
CHEMBL1241578 IC50 = 100.0 nM 7.00
CHEMBL1242202 IC50 = 113.0 nM 6.95
CHEMBL1242386 IC50 = 113.0 nM 6.95
CHEMBL1240554 IC50 = 116.0 nM 6.94
CHEMBL1242028 IC50 = 118.0 nM 6.93
CHEMBL1242201 IC50 = 120.0 nM 6.92
CHEMBL1242294 IC50 = 123.0 nM 6.91
CHEMBL1242666 IC50 = 140.0 nM 6.85
CHEMBL1241484 IC50 = 140.0 nM 6.85
CHEMBL1241676 IC50 = 147.0 nM 6.83
CHEMBL1242208 IC50 = 167.0 nM 6.78
CHEMBL1241683 IC50 = 184.0 nM 6.74
CHEMBL1241945 IC50 = 187.0 nM 6.73
CHEMBL1242112 IC50 = 190.0 nM 6.72
CHEMBL1242290 IC50 = 200.0 nM 6.70
CHEMBL1241301 IC50 = 200.0 nM 6.70
CHEMBL1241767 IC50 = 200.0 nM 6.70
CHEMBL1242377 IC50 = 209.0 nM 6.68
CHEMBL1242756 IC50 = 220.0 nM 6.66
CHEMBL1242209 IC50 = 228.0 nM 6.64
CHEMBL1241491 IC50 = 239.0 nM 6.62
CHEMBL1241949 IC50 = 242.0 nM 6.62
CHEMBL1242568 IC50 = 257.0 nM 6.59
CHEMBL1242285 IC50 = 270.0 nM 6.57
CHEMBL1241581 IC50 = 271.0 nM 6.57
CHEMBL1242656 IC50 = 283.0 nM 6.55
CHEMBL1241580 IC50 = 293.0 nM 6.53
CHEMBL1242569 IC50 = 311.0 nM 6.51
CHEMBL1242477 IC50 = 330.0 nM 6.48
CHEMBL1242198 IC50 = 340.0 nM 6.47
CHEMBL1242114 IC50 = 340.0 nM 6.47
CHEMBL1242749 IC50 = 342.0 nM 6.47
CHEMBL1241490 IC50 = 347.0 nM 6.46
CHEMBL1242659 IC50 = 353.0 nM 6.45
CHEMBL1242113 IC50 = 355.0 nM 6.45