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Assay Detail

CHEMBL4387673

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Binding
Inhibition of PI3KD (unknown origin) by HTRF assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow.
Fradera X, Methot JL, Achab A, Christopher M, Altman MD, Zhou H, McGowan MA, Kattar SD, Wilson K, Garcia Y, Augustin MA, Lesburg CA, Shah S, Goldenblatt P, Katz JD.
Bioorg Med Chem Lett (2019) 29 : 2575 -2580
PubMed 31416665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.42 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4434674 1 9.48
CHEMBL4452905 1 9.00
CHEMBL4449778 1 8.72
CHEMBL4517406 1 8.14
CHEMBL4524356 1 8.00
CHEMBL4575776 1 8.00
CHEMBL4440095 1 7.96
CHEMBL4474516 1 7.92
CHEMBL4461221 1 7.70
CHEMBL4515312 1 7.64
CHEMBL4562428 1 7.62
CHEMBL4549113 1 7.57
CHEMBL4435654 1 7.50
CHEMBL4436827 1 7.48
CHEMBL4522603 1 7.47
CHEMBL4451433 1 7.43
CHEMBL4586842 1 7.37
CHEMBL4475748 1 7.24
CHEMBL4438805 1 7.22
CHEMBL4562183 1 7.21
CHEMBL4456087 1 7.05
CHEMBL4452117 1 7.03
CHEMBL4468849 1 6.82
CHEMBL4471570 1 6.75
CHEMBL4549128 1 6.75
CHEMBL4447681 1 6.46
CHEMBL4435568 1 6.43
CHEMBL4455359 1 6.28
CHEMBL4436565 1 6.27
CHEMBL4444468 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4434674 IC50 = 0.33 nM 9.48
CHEMBL4452905 IC50 = 1.0 nM 9.00
CHEMBL4449778 IC50 = 1.9 nM 8.72
CHEMBL4517406 IC50 = 7.2 nM 8.14
CHEMBL4524356 IC50 = 10.0 nM 8.00
CHEMBL4575776 IC50 = 10.0 nM 8.00
CHEMBL4440095 IC50 = 11.0 nM 7.96
CHEMBL4474516 IC50 = 12.0 nM 7.92
CHEMBL4461221 IC50 = 20.0 nM 7.70
CHEMBL4515312 IC50 = 23.0 nM 7.64
CHEMBL4562428 IC50 = 24.0 nM 7.62
CHEMBL4549113 IC50 = 27.0 nM 7.57
CHEMBL4435654 IC50 = 32.0 nM 7.50
CHEMBL4436827 IC50 = 33.0 nM 7.48
CHEMBL4522603 IC50 = 34.0 nM 7.47
CHEMBL4451433 IC50 = 37.0 nM 7.43
CHEMBL4586842 IC50 = 43.0 nM 7.37
CHEMBL4475748 IC50 = 58.0 nM 7.24
CHEMBL4438805 IC50 = 60.0 nM 7.22
CHEMBL4562183 IC50 = 61.0 nM 7.21
CHEMBL4456087 IC50 = 89.0 nM 7.05
CHEMBL4452117 IC50 = 94.0 nM 7.03
CHEMBL4468849 IC50 = 150.0 nM 6.82
CHEMBL4471570 IC50 = 180.0 nM 6.75
CHEMBL4549128 IC50 = 179.0 nM 6.75
CHEMBL4447681 IC50 = 343.0 nM 6.46
CHEMBL4435568 IC50 = 374.0 nM 6.43
CHEMBL4455359 IC50 = 530.0 nM 6.28
CHEMBL4436565 IC50 = 540.0 nM 6.27
CHEMBL4444468 IC50 = 689.0 nM 6.16
CHEMBL4454950 IC50 > 10000.0 nM -