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Assay Detail

CHEMBL4818576

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

Binding
Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assay
28
Total Activities
28
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

Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds.
Vara BA, Levi SM, Achab A, Candito DA, Fradera X, Lesburg CA, Kawamura S, Lacey BM, Lim J, Methot JL, Xu Z, Xu H, Smith DM, Piesvaux JA, Miller JR, Bittinger M, Ranganath SH, Bennett DJ, DiMauro EF, Pasternak A.
ACS Med Chem Lett (2021) 12 : 653 -661
PubMed 33859804 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 9.39 10.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4870155 1 10.57
CHEMBL4864568 1 10.43
CHEMBL4848845 1 10.43
CHEMBL4866139 1 10.28
CHEMBL4865305 1 10.21
CHEMBL4855158 1 10.17
CHEMBL4863492 1 10.03
CHEMBL4872743 1 9.96
CHEMBL4866616 1 9.89
CHEMBL4879259 1 9.80
CHEMBL4860645 1 9.80
CHEMBL4849567 1 9.70
CHEMBL4857184 1 9.66
CHEMBL4878586 1 9.60
CHEMBL4874375 1 9.59
CHEMBL4871382 1 9.54
CHEMBL4873035 1 9.52
CHEMBL4859773 1 9.34
CHEMBL4851277 1 9.23
CHEMBL4868682 1 9.16
CHEMBL4868487 1 9.06
CHEMBL4878650 1 8.36
CHEMBL4860928 1 8.11
CHEMBL4873991 1 8.08
CHEMBL4856183 1 7.94
CHEMBL4876320 1 7.85
CHEMBL4868527 1 7.19
CHEMBL4859451 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4870155 IC50 = 0.027 nM 10.57
CHEMBL4864568 IC50 = 0.037 nM 10.43
CHEMBL4848845 IC50 = 0.037 nM 10.43
CHEMBL4866139 IC50 = 0.052 nM 10.28
CHEMBL4865305 IC50 = 0.061 nM 10.21
CHEMBL4855158 IC50 = 0.067 nM 10.17
CHEMBL4863492 IC50 = 0.094 nM 10.03
CHEMBL4872743 IC50 = 0.11 nM 9.96
CHEMBL4866616 IC50 = 0.13 nM 9.89
CHEMBL4879259 IC50 = 0.16 nM 9.80
CHEMBL4860645 IC50 = 0.16 nM 9.80
CHEMBL4849567 IC50 = 0.2 nM 9.70
CHEMBL4857184 IC50 = 0.22 nM 9.66
CHEMBL4878586 IC50 = 0.25 nM 9.60
CHEMBL4874375 IC50 = 0.26 nM 9.59
CHEMBL4871382 IC50 = 0.29 nM 9.54
CHEMBL4873035 IC50 = 0.3 nM 9.52
CHEMBL4859773 IC50 = 0.46 nM 9.34
CHEMBL4851277 IC50 = 0.59 nM 9.23
CHEMBL4868682 IC50 = 0.69 nM 9.16
CHEMBL4868487 IC50 = 0.88 nM 9.06
CHEMBL4878650 IC50 = 4.4 nM 8.36
CHEMBL4860928 IC50 = 7.7 nM 8.11
CHEMBL4873991 IC50 = 8.3 nM 8.08
CHEMBL4856183 IC50 = 11.4 nM 7.94
CHEMBL4876320 IC50 = 14.0 nM 7.85
CHEMBL4868527 IC50 = 64.0 nM 7.19
CHEMBL4859451 IC50 = 0.005 nM -