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Assay Detail

CHEMBL4839698

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

Binding
Inhibition of human recombinant ARG1 expressed in Escherichia coli using thioarginine as a substrate preincubated for 30 mins followed by substrate addition and incubated for 60 mins by fluorescence based arginine thio ornithine generating 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

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
IC50 31 7.22 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4850213 1 8.70
CHEMBL4763578 1 8.52
CHEMBL4778978 1 8.40
CHEMBL4852406 1 8.30
CHEMBL4864502 1 8.30
CHEMBL4868283 1 8.15
CHEMBL4872801 1 8.10
CHEMBL4875641 1 7.96
CHEMBL4858437 1 7.80
CHEMBL4855923 1 7.72
CHEMBL4863489 1 7.70
CHEMBL4845882 1 7.54
CHEMBL4862990 1 7.52
CHEMBL4876150 1 7.48
CHEMBL4856276 1 7.47
CHEMBL4862982 1 7.34
CHEMBL4868849 1 7.18
CHEMBL4871410 1 7.16
CHEMBL4855854 1 6.94
CHEMBL4867493 1 6.92
CHEMBL4853323 1 6.68
CHEMBL4848931 1 6.61
CHEMBL1812661 1 6.51
CHEMBL4851360 1 6.47
CHEMBL4870874 1 6.42
CHEMBL4863179 1 6.38
CHEMBL4856326 1 6.35
CHEMBL4863141 1 6.18
CHEMBL4875190 1 5.06
CHEMBL4853009 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4850213 IC50 = 2.0 nM 8.70
CHEMBL4763578 IC50 = 3.0 nM 8.52
CHEMBL4778978 IC50 = 4.0 nM 8.40
CHEMBL4852406 IC50 = 5.0 nM 8.30
CHEMBL4864502 IC50 = 5.0 nM 8.30
CHEMBL4868283 IC50 = 7.0 nM 8.15
CHEMBL4872801 IC50 = 8.0 nM 8.10
CHEMBL4875641 IC50 = 11.0 nM 7.96
CHEMBL4858437 IC50 = 16.0 nM 7.80
CHEMBL4855923 IC50 = 19.0 nM 7.72
CHEMBL4863489 IC50 = 20.0 nM 7.70
CHEMBL4845882 IC50 = 29.0 nM 7.54
CHEMBL4862990 IC50 = 30.0 nM 7.52
CHEMBL4876150 IC50 = 33.0 nM 7.48
CHEMBL4856276 IC50 = 34.0 nM 7.47
CHEMBL4862982 IC50 = 46.0 nM 7.34
CHEMBL4868849 IC50 = 66.0 nM 7.18
CHEMBL4871410 IC50 = 70.0 nM 7.16
CHEMBL4855854 IC50 = 114.0 nM 6.94
CHEMBL4867493 IC50 = 120.0 nM 6.92
CHEMBL4853323 IC50 = 211.0 nM 6.68
CHEMBL4848931 IC50 = 247.0 nM 6.61
CHEMBL1812661 IC50 = 311.0 nM 6.51
CHEMBL4851360 IC50 = 340.0 nM 6.47
CHEMBL4870874 IC50 = 377.0 nM 6.42
CHEMBL4863179 IC50 = 413.0 nM 6.38
CHEMBL4856326 IC50 = 447.0 nM 6.35
CHEMBL4863141 IC50 = 660.0 nM 6.18
CHEMBL4875190 IC50 = 8733.0 nM 5.06
CHEMBL4853009 IC50 = 19840.0 nM 4.70
CHEMBL4748950 IC50 < 1.0 nM -