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Assay Detail

CHEMBL1243966

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

Binding
Inhibition of recombinant PI3Kbeta by radioactive phosphotransfer assay in presence of 10 uM ATP
206
Total Activities
206
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 206 5.23 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1233881 1 6.89
CHEMBL1242470 1 6.77
CHEMBL1241299 1 6.76
CHEMBL1241301 1 6.67
CHEMBL1242290 1 6.64
CHEMBL1242287 1 6.63
CHEMBL1240553 1 6.63
CHEMBL1241578 1 6.62
CHEMBL1233882 1 6.62
CHEMBL1242285 1 6.59
CHEMBL1242201 1 6.58
CHEMBL1240554 1 6.53
CHEMBL1242376 1 6.50
CHEMBL1242198 1 6.46
CHEMBL1242199 1 6.46
CHEMBL1242567 1 6.44
CHEMBL1241241 1 6.42
CHEMBL1242657 1 6.37
CHEMBL1241492 1 6.36
CHEMBL1241776 1 6.33
CHEMBL1242469 1 6.32
CHEMBL1242209 1 6.32
CHEMBL1242752 1 6.31
CHEMBL1241949 1 6.30
CHEMBL1242379 1 6.28
CHEMBL1241678 1 6.26
CHEMBL1242386 1 6.26
CHEMBL1242573 1 6.26
CHEMBL1242377 1 6.21
CHEMBL1241484 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1233881 IC50 = 130.0 nM 6.89
CHEMBL1242470 IC50 = 169.0 nM 6.77
CHEMBL1241299 IC50 = 173.0 nM 6.76
CHEMBL1241301 IC50 = 216.0 nM 6.67
CHEMBL1242290 IC50 = 230.0 nM 6.64
CHEMBL1242287 IC50 = 235.0 nM 6.63
CHEMBL1240553 IC50 = 232.0 nM 6.63
CHEMBL1241578 IC50 = 240.0 nM 6.62
CHEMBL1233882 IC50 = 240.0 nM 6.62
CHEMBL1242285 IC50 = 255.0 nM 6.59
CHEMBL1242201 IC50 = 261.0 nM 6.58
CHEMBL1240554 IC50 = 294.0 nM 6.53
CHEMBL1242376 IC50 = 320.0 nM 6.50
CHEMBL1242199 IC50 = 343.0 nM 6.46
CHEMBL1242198 IC50 = 350.0 nM 6.46
CHEMBL1242567 IC50 = 364.0 nM 6.44
CHEMBL1241241 IC50 = 380.0 nM 6.42
CHEMBL1242657 IC50 = 432.0 nM 6.37
CHEMBL1241492 IC50 = 440.0 nM 6.36
CHEMBL1241776 IC50 = 467.0 nM 6.33
CHEMBL1242469 IC50 = 481.0 nM 6.32
CHEMBL1242209 IC50 = 476.0 nM 6.32
CHEMBL1242752 IC50 = 492.0 nM 6.31
CHEMBL1241949 IC50 = 500.0 nM 6.30
CHEMBL1242379 IC50 = 525.0 nM 6.28
CHEMBL1242386 IC50 = 550.0 nM 6.26
CHEMBL1241678 IC50 = 550.0 nM 6.26
CHEMBL1242573 IC50 = 548.0 nM 6.26
CHEMBL1242377 IC50 = 613.0 nM 6.21
CHEMBL1242476 IC50 = 658.0 nM 6.18
CHEMBL1241484 IC50 = 660.0 nM 6.18
CHEMBL1241767 IC50 = 670.0 nM 6.17
CHEMBL1242114 IC50 = 697.0 nM 6.16
CHEMBL1242749 IC50 = 715.0 nM 6.15
CHEMBL1241944 IC50 = 742.0 nM 6.13
CHEMBL1241768 IC50 = 809.0 nM 6.09
CHEMBL1242113 IC50 = 809.0 nM 6.09
CHEMBL1242384 IC50 = 854.0 nM 6.07
CHEMBL1241677 IC50 = 864.0 nM 6.06
CHEMBL1241676 IC50 = 941.0 nM 6.03
CHEMBL1241770 IC50 = 962.0 nM 6.02
CHEMBL1242202 IC50 = 949.0 nM 6.02
CHEMBL1241774 IC50 = 975.0 nM 6.01
CHEMBL1242477 IC50 = 1000.0 nM 6.00
CHEMBL1242293 IC50 = 1000.0 nM 6.00
CHEMBL1242568 IC50 = 1020.0 nM 5.99
CHEMBL1242119 IC50 = 1100.0 nM 5.96
CHEMBL1242385 IC50 = 1100.0 nM 5.96
CHEMBL1242656 IC50 = 1240.0 nM 5.91
CHEMBL1242027 IC50 = 1280.0 nM 5.89