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Assay Detail

CHEMBL4839701

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

Binding
Inhibition of human ARG1 in HEK293 cells by cell based assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Arginase-1 (CHEMBL1075097)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology.
Lu M, Zhang H, Li D, Childers M, Pu Q, Palte RL, Gathiaka S, Lyons TW, Palani A, Fan PW, Spacciapoli P, Miller JR, Cho H, Cheng M, Chakravarthy K, O'Neil J, Eangoor P, Beard A, Kim HY, Saurí J, Gunaydin H, Sloman DL, Siliphaivanh P, Cumming J, Fischer C.
ACS Med Chem Lett (2021) 12 : 1380 -1388
PubMed 34527178 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 5.06 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4868283 1 5.55
CHEMBL4858437 1 5.47
CHEMBL4872801 1 5.38
CHEMBL4876150 1 5.20
CHEMBL4778978 1 5.16
CHEMBL4855923 1 4.96
CHEMBL4852406 1 4.85
CHEMBL4862990 1 4.80
CHEMBL4763578 1 4.70
CHEMBL4862982 1 4.55
CHEMBL4871410 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4868283 EC50 = 2800.0 nM 5.55
CHEMBL4858437 EC50 = 3400.0 nM 5.47
CHEMBL4872801 EC50 = 4200.0 nM 5.38
CHEMBL4876150 EC50 = 6300.0 nM 5.20
CHEMBL4778978 EC50 = 6900.0 nM 5.16
CHEMBL4855923 EC50 = 11000.0 nM 4.96
CHEMBL4852406 EC50 = 14000.0 nM 4.85
CHEMBL4862990 EC50 = 16000.0 nM 4.80
CHEMBL4763578 EC50 = 20000.0 nM 4.70
CHEMBL4862982 EC50 = 28000.0 nM 4.55
CHEMBL4871410 EC50 > 30000.0 nM -