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Assay Detail

CHEMBL1680108

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Binding
Inhibition of PI3Kalpha after 15 mins
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors.
Burger MT, Knapp M, Wagman A, Ni ZJ, Hendrickson T, Atallah G, Zhang Y, Frazier K, Verhagen J, Pfister K, Ng S, Smith A, Bartulis S, Merrit H, Weismann M, Xin X, Haznedar J, Voliva CF, Iwanowicz E, Pecchi S.
ACS Med Chem Lett (2011) 2 : 34 -38
PubMed 24900252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.29 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1672329 1 8.22
CHEMBL1672324 1 8.15
CHEMBL1672321 1 8.10
CHEMBL1672330 1 7.89
CHEMBL1672331 1 7.85
CHEMBL1672320 1 7.36
CHEMBL1672316 1 7.26
CHEMBL1672314 1 7.21
CHEMBL1672317 1 7.18
CHEMBL1672315 1 6.87
CHEMBL1672319 1 6.64
CHEMBL1672325 1 6.61
CHEMBL1672318 1 6.60
CHEMBL1672322 1 6.11
CHEMBL1672323 1 -
CHEMBL1672326 1 -
CHEMBL1672327 1 -
CHEMBL1672328 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1672329 IC50 = 6.0 nM 8.22
CHEMBL1672324 IC50 = 7.0 nM 8.15
CHEMBL1672321 IC50 = 8.0 nM 8.10
CHEMBL1672330 IC50 = 13.0 nM 7.89
CHEMBL1672331 IC50 = 14.0 nM 7.85
CHEMBL1672320 IC50 = 44.0 nM 7.36
CHEMBL1672316 IC50 = 55.0 nM 7.26
CHEMBL1672314 IC50 = 61.0 nM 7.21
CHEMBL1672317 IC50 = 66.0 nM 7.18
CHEMBL1672315 IC50 = 135.0 nM 6.87
CHEMBL1672319 IC50 = 231.0 nM 6.64
CHEMBL1672325 IC50 = 247.0 nM 6.61
CHEMBL1672318 IC50 = 253.0 nM 6.60
CHEMBL1672322 IC50 = 774.0 nM 6.11
CHEMBL1672323 IC50 < 2.0 nM -
CHEMBL1672326 IC50 < 2.0 nM -
CHEMBL1672327 IC50 < 2.0 nM -
CHEMBL1672328 IC50 < 2.0 nM -