Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4337249

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

Binding
Inhibition of human recombinant arginase 1 expressed in Escherichia coli BL21 (DE3) assessed as reduction in urea production using L-arginine as substrate in presence of MnSO4 incubated for 60 mins by o-phthaldialdehyde/N-(1-naphthyl)ethylene-diamine dihydrochloride reagent based colorimetric assay
29
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

Target

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

Publication

Discovery of <i>N</i>-Substituted 3-Amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic Acids as Highly Potent Third-Generation Inhibitors of Human Arginase I and II.
Van Zandt MC, Jagdmann GE, Whitehouse DL, Ji M, Savoy J, Potapova O, Cousido-Siah A, Mitschler A, Howard EI, Pyle AM, Podjarny AD.
J Med Chem (2019) 62 : 8164 -8177
PubMed 31408339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.05 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4538713 1 8.89
CHEMBL4450972 1 8.60
CHEMBL4557975 1 8.59
CHEMBL4518246 1 8.11
CHEMBL4594157 1 8.00
CHEMBL4572850 1 8.00
CHEMBL4461464 1 8.00
CHEMBL4578964 1 7.96
CHEMBL4530103 1 7.80
CHEMBL4459462 1 7.75
CHEMBL4556601 1 7.72
CHEMBL4434802 1 7.52
CHEMBL4573202 1 7.00
CHEMBL4553794 1 6.96
CHEMBL4440992 1 6.68
CHEMBL4576356 1 6.52
CHEMBL4590074 1 6.47
CHEMBL4461151 1 6.44
CHEMBL4457401 1 6.42
CHEMBL4546530 2 6.42
CHEMBL4565795 1 6.41
CHEMBL4547509 1 6.40
CHEMBL4469486 1 6.33
CHEMBL4444238 1 6.22
CHEMBL4467506 1 6.17
CHEMBL1234777 NOR-NOHA 1.0 1 5.87
CHEMBL1812661 1 5.81
CHEMBL4514628 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4538713 IC50 = 1.3 nM 8.89
CHEMBL4450972 IC50 = 2.5 nM 8.60
CHEMBL4557975 IC50 = 2.6 nM 8.59
CHEMBL4518246 IC50 = 7.7 nM 8.11
CHEMBL4594157 IC50 = 10.0 nM 8.00
CHEMBL4572850 IC50 = 10.0 nM 8.00
CHEMBL4461464 IC50 = 10.0 nM 8.00
CHEMBL4578964 IC50 = 11.0 nM 7.96
CHEMBL4530103 IC50 = 16.0 nM 7.80
CHEMBL4459462 IC50 = 18.0 nM 7.75
CHEMBL4556601 IC50 = 19.0 nM 7.72
CHEMBL4434802 IC50 = 30.0 nM 7.52
CHEMBL4573202 IC50 = 100.0 nM 7.00
CHEMBL4553794 IC50 = 110.0 nM 6.96
CHEMBL4440992 IC50 = 210.0 nM 6.68
CHEMBL4576356 IC50 = 300.0 nM 6.52
CHEMBL4590074 IC50 = 340.0 nM 6.47
CHEMBL4461151 IC50 = 360.0 nM 6.44
CHEMBL4457401 IC50 = 380.0 nM 6.42
CHEMBL4546530 IC50 = 380.0 nM 6.42
CHEMBL4565795 IC50 = 390.0 nM 6.41
CHEMBL4547509 IC50 = 400.0 nM 6.40
CHEMBL4469486 IC50 = 470.0 nM 6.33
CHEMBL4444238 IC50 = 600.0 nM 6.22
CHEMBL4467506 IC50 = 670.0 nM 6.17
CHEMBL1234777 NOR-NOHA IC50 = 1360.0 nM 5.87
CHEMBL1812661 IC50 = 1547.0 nM 5.81
CHEMBL4546530 IC50 = 48000.0 nM 4.32
CHEMBL4514628 IC50 - -