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Assay Detail

CHEMBL4605919

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

Binding
Inhibition of human arginase1 in presence of DNTB by thio ornithine generation assay
35
Total Activities
35
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

Discovery and Optimization of Rationally Designed Bicyclic Inhibitors of Human Arginase to Enhance Cancer Immunotherapy.
Mitcheltree MJ, Li D, Achab A, Beard A, Chakravarthy K, Cheng M, Cho H, Eangoor P, Fan P, Gathiaka S, Kim HY, Lesburg CA, Lyons TW, Martinot TA, Miller JR, McMinn S, O'Neil J, Palani A, Palte RL, Saurí J, Sloman DL, Zhang H, Cumming JN, Fischer C.
ACS Med Chem Lett (2020) 11 : 582 -588
PubMed 32292567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 7.15 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4639893 1 8.40
CHEMBL4640681 1 8.30
CHEMBL4648504 1 8.15
CHEMBL4633222 1 7.92
CHEMBL4646013 1 7.89
CHEMBL4632493 1 7.85
CHEMBL4633123 1 7.85
CHEMBL4440992 1 7.85
CHEMBL2326089 1 7.75
CHEMBL4647529 1 7.70
CHEMBL4648095 1 7.66
CHEMBL4632821 1 7.64
CHEMBL4639162 1 7.54
CHEMBL4639122 1 7.48
CHEMBL4639443 1 7.43
CHEMBL4632863 1 7.37
CHEMBL4636445 1 7.37
CHEMBL4646697 1 7.28
CHEMBL4637242 1 7.09
CHEMBL4639175 1 7.08
CHEMBL4647364 1 6.97
CHEMBL4553794 1 6.95
CHEMBL4643311 1 6.80
CHEMBL4637540 1 6.75
CHEMBL4647269 1 6.75
CHEMBL4645115 1 6.66
CHEMBL4643670 1 6.62
CHEMBL4643616 1 6.60
CHEMBL4638362 1 6.59
CHEMBL1812661 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4639893 IC50 = 4.0 nM 8.40
CHEMBL4640681 IC50 = 5.0 nM 8.30
CHEMBL4648504 IC50 = 7.0 nM 8.15
CHEMBL4633222 IC50 = 12.0 nM 7.92
CHEMBL4646013 IC50 = 13.0 nM 7.89
CHEMBL4632493 IC50 = 14.0 nM 7.85
CHEMBL4633123 IC50 = 14.0 nM 7.85
CHEMBL4440992 IC50 = 14.0 nM 7.85
CHEMBL2326089 IC50 = 18.0 nM 7.75
CHEMBL4647529 IC50 = 20.0 nM 7.70
CHEMBL4648095 IC50 = 22.0 nM 7.66
CHEMBL4632821 IC50 = 23.0 nM 7.64
CHEMBL4639162 IC50 = 29.0 nM 7.54
CHEMBL4639122 IC50 = 33.0 nM 7.48
CHEMBL4639443 IC50 = 37.0 nM 7.43
CHEMBL4632863 IC50 = 43.0 nM 7.37
CHEMBL4636445 IC50 = 43.0 nM 7.37
CHEMBL4646697 IC50 = 52.0 nM 7.28
CHEMBL4637242 IC50 = 81.0 nM 7.09
CHEMBL4639175 IC50 = 83.0 nM 7.08
CHEMBL4647364 IC50 = 108.0 nM 6.97
CHEMBL4553794 IC50 = 113.0 nM 6.95
CHEMBL4643311 IC50 = 160.0 nM 6.80
CHEMBL4637540 IC50 = 178.0 nM 6.75
CHEMBL4647269 IC50 = 179.0 nM 6.75
CHEMBL4645115 IC50 = 220.0 nM 6.66
CHEMBL4643670 IC50 = 237.0 nM 6.62
CHEMBL4643616 IC50 = 252.0 nM 6.60
CHEMBL4638362 IC50 = 259.0 nM 6.59
CHEMBL1812661 IC50 = 311.0 nM 6.51
CHEMBL4638209 IC50 = 522.0 nM 6.28
CHEMBL4636066 IC50 = 529.0 nM 6.28
CHEMBL4647330 IC50 = 1212.0 nM 5.92
CHEMBL4642576 IC50 = 2630.0 nM 5.58
CHEMBL4635957 IC50 = 5273.0 nM 5.28