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Assay Detail

CHEMBL5538899

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 L-arginine hydrochloride as substrate assessed as inhibition of urea production incubated for 20 mins by colorimetric analysis
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

Novel orally bioavailable piperidine derivatives as extracellular arginase inhibitors developed by a ring expansion.
Gzik A, Borek B, Chrzanowski J, Jedrzejczak K, Dziegielewski M, Brzezinska J, Nowicka J, Grzybowski MM, Rejczak T, Niedzialek D, Wieczorek G, Olczak J, Golebiowski A, Zaslona Z, Blaszczyk R.
Eur J Med Chem (2024) 264 : 116033 -116033
PubMed 38096651 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.42 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5572458 1 7.70
CHEMBL5573574 1 6.80
CHEMBL5564694 1 6.68
CHEMBL5590630 1 6.62
CHEMBL4749434 1 6.60
CHEMBL5574058 1 6.60
CHEMBL5584145 1 6.60
CHEMBL5569448 1 6.57
CHEMBL5569123 1 6.55
CHEMBL5564404 1 6.55
CHEMBL5592979 1 6.55
CHEMBL5573132 1 6.51
CHEMBL5574720 1 6.47
CHEMBL5570988 1 6.46
CHEMBL5569035 1 6.44
CHEMBL5572916 1 6.44
CHEMBL5570457 1 6.44
CHEMBL5579689 1 6.42
CHEMBL5573227 1 6.40
CHEMBL5570085 1 6.40
CHEMBL5566718 1 6.38
CHEMBL5575750 1 6.38
CHEMBL5567616 1 6.21
CHEMBL5569670 1 6.19
CHEMBL5593553 1 6.17
CHEMBL5574724 1 6.13
CHEMBL5562980 1 6.12
CHEMBL5563536 1 6.12
CHEMBL5574905 1 6.08
CHEMBL5573192 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5572458 IC50 = 20.0 nM 7.70
CHEMBL5573574 IC50 = 160.0 nM 6.80
CHEMBL5564694 IC50 = 210.0 nM 6.68
CHEMBL5590630 IC50 = 240.0 nM 6.62
CHEMBL4749434 IC50 = 250.0 nM 6.60
CHEMBL5574058 IC50 = 250.0 nM 6.60
CHEMBL5584145 IC50 = 250.0 nM 6.60
CHEMBL5569448 IC50 = 270.0 nM 6.57
CHEMBL5569123 IC50 = 280.0 nM 6.55
CHEMBL5564404 IC50 = 280.0 nM 6.55
CHEMBL5592979 IC50 = 280.0 nM 6.55
CHEMBL5573132 IC50 = 310.0 nM 6.51
CHEMBL5574720 IC50 = 340.0 nM 6.47
CHEMBL5570988 IC50 = 350.0 nM 6.46
CHEMBL5570457 IC50 = 360.0 nM 6.44
CHEMBL5569035 IC50 = 360.0 nM 6.44
CHEMBL5572916 IC50 = 360.0 nM 6.44
CHEMBL5579689 IC50 = 380.0 nM 6.42
CHEMBL5570085 IC50 = 400.0 nM 6.40
CHEMBL5573227 IC50 = 400.0 nM 6.40
CHEMBL5566718 IC50 = 420.0 nM 6.38
CHEMBL5575750 IC50 = 420.0 nM 6.38
CHEMBL5567616 IC50 = 610.0 nM 6.21
CHEMBL5569670 IC50 = 650.0 nM 6.19
CHEMBL5593553 IC50 = 680.0 nM 6.17
CHEMBL5574724 IC50 = 740.0 nM 6.13
CHEMBL5562980 IC50 = 760.0 nM 6.12
CHEMBL5563536 IC50 = 760.0 nM 6.12
CHEMBL5574905 IC50 = 830.0 nM 6.08
CHEMBL5573192 IC50 = 1200.0 nM 5.92
CHEMBL5574669 IC50 = 3220.0 nM 5.49
CHEMBL5562639 IC50 > 10000.0 nM -
CHEMBL5573103 IC50 > 10000.0 nM -
CHEMBL5591050 IC50 > 10000.0 nM -
CHEMBL5565043 IC50 > 10000.0 nM -