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Assay Detail

CHEMBL5737474

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

Binding
PI3Kdelta Inhibition Assay: The IC50s obtained by the method of Assay A at 1 mM ATP as described in the US Patent Publications.
33
Total Activities
8
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Pyrrolopyrimidine derivatives as TAM inhibitors
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.97 7.12
kon 11 - -
k_off 11 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4576207 3 7.12
CHEMBL6026135 12 6.90
CHEMBL5775827 3 -
CHEMBL2216863 DEZAPELISIB 2.0 3 -
CHEMBL5776309 3 -
CHEMBL5779126 3 -
CHEMBL5773238 3 -
CHEMBL2216867 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4576207 IC50 = 75.0 nM 7.12
CHEMBL6026135 IC50 = 125.0 nM 6.90
CHEMBL6026135 IC50 = 125.0 nM 6.90
CHEMBL5775827 IC50 < 50.0 nM -
CHEMBL5775827 kon = - -
CHEMBL5773238 k_off = - s-1 -
CHEMBL5773238 kon = - -
CHEMBL5773238 IC50 < 50.0 nM -
CHEMBL5779126 k_off = - s-1 -
CHEMBL5779126 kon = - -
CHEMBL5779126 IC50 < 50.0 nM -
CHEMBL5776309 k_off = - s-1 -
CHEMBL5776309 kon = - -
CHEMBL5776309 IC50 < 50.0 nM -
CHEMBL2216863 DEZAPELISIB k_off = - s-1 -
CHEMBL2216863 DEZAPELISIB kon = - -
CHEMBL2216863 DEZAPELISIB IC50 < 50.0 nM -
CHEMBL5775827 k_off = - s-1 -
CHEMBL6026135 k_off = - s-1 -
CHEMBL4576207 k_off = - s-1 -
CHEMBL4576207 kon = - -
CHEMBL2216867 k_off = - s-1 -
CHEMBL2216867 kon = - -
CHEMBL2216867 IC50 < 50.0 nM -
CHEMBL6026135 k_off = - s-1 -
CHEMBL6026135 kon = - -
CHEMBL6026135 k_off = - s-1 -
CHEMBL6026135 kon = - -
CHEMBL6026135 IC50 < 50.0 nM -
CHEMBL6026135 k_off = - s-1 -
CHEMBL6026135 kon = - -
CHEMBL6026135 IC50 < 50.0 nM -
CHEMBL6026135 kon = - -