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Assay Detail

CHEMBL5735101

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Binding
Inhibition Assay: Inhibition of arginase I (ARG I) and arginase II (ARG II) by Formula I or Formula II compounds is followed spectrophotometrically at 530 nm. The compound to be tested was dissolved in DMSO at an initial concentration 50-fold greater than its final concentration in the cuvette. 10 μl of the stock solution was diluted in 90 μl of the assay buffer that comprises 0.1M sodium phosphate buffer containing 130 mM NaCl, pH 7.4, to which is added ovalbumin (OVA) at a concentration of 1 mg/ml. Solutions of arginase I and II were prepared in 100 mM sodium phosphate buffer, pH 7.4 containing 1 mg/ml of OVA to give an arginase stock solution at a final concentration of 100 ng/ml.
195
Total Activities
64
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Arginase-2, mitochondrial (CHEMBL1795148)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Arginase inhibitors as therapeutics
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 5.74 6.00
kon 65 - -
k_off 65 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6026515 3 6.00
CHEMBL6012978 3 6.00
CHEMBL5908795 3 6.00
CHEMBL5938641 3 6.00
CHEMBL5963426 3 6.00
CHEMBL6038642 3 6.00
CHEMBL6009975 3 6.00
CHEMBL5801265 3 6.00
CHEMBL5945319 3 6.00
CHEMBL6011997 3 6.00
CHEMBL6030393 3 6.00
CHEMBL5806072 3 6.00
CHEMBL5749833 3 6.00
CHEMBL5910912 3 6.00
CHEMBL5850215 3 6.00
CHEMBL5958196 3 6.00
CHEMBL5744965 3 6.00
CHEMBL5847950 3 6.00
CHEMBL5899394 3 6.00
CHEMBL5945202 3 6.00
CHEMBL5837269 6 6.00
CHEMBL5875670 3 5.70
CHEMBL5956917 3 5.70
CHEMBL6058456 3 5.70
CHEMBL5863488 3 5.70
CHEMBL5929671 3 5.70
CHEMBL5743998 3 5.70
CHEMBL5748082 3 5.70
CHEMBL5819053 3 5.70
CHEMBL5902643 3 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5837269 IC50 = 1000.0 nM 6.00
CHEMBL5910912 IC50 = 1000.0 nM 6.00
CHEMBL6030393 IC50 = 1000.0 nM 6.00
CHEMBL5801265 IC50 = 1000.0 nM 6.00
CHEMBL6009975 IC50 = 1000.0 nM 6.00
CHEMBL5806072 IC50 = 1000.0 nM 6.00
CHEMBL5837269 IC50 = 1000.0 nM 6.00
CHEMBL5958196 IC50 = 1000.0 nM 6.00
CHEMBL5945319 IC50 = 1000.0 nM 6.00
CHEMBL5847950 IC50 = 1000.0 nM 6.00
CHEMBL6038642 IC50 = 1000.0 nM 6.00
CHEMBL5945202 IC50 = 1000.0 nM 6.00
CHEMBL5850215 IC50 = 1000.0 nM 6.00
CHEMBL6011997 IC50 = 1000.0 nM 6.00
CHEMBL5899394 IC50 = 1000.0 nM 6.00
CHEMBL5908795 IC50 = 1000.0 nM 6.00
CHEMBL5749833 IC50 = 1000.0 nM 6.00
CHEMBL5938641 IC50 = 1000.0 nM 6.00
CHEMBL5744965 IC50 = 1000.0 nM 6.00
CHEMBL6026515 IC50 = 1000.0 nM 6.00
CHEMBL6012978 IC50 = 1000.0 nM 6.00
CHEMBL5963426 IC50 = 1000.0 nM 6.00
CHEMBL5751054 IC50 = 2000.0 nM 5.70
CHEMBL5863488 IC50 = 2000.0 nM 5.70
CHEMBL4440992 IC50 = 2000.0 nM 5.70
CHEMBL5748082 IC50 = 2000.0 nM 5.70
CHEMBL5890848 IC50 = 2000.0 nM 5.70
CHEMBL6058456 IC50 = 2000.0 nM 5.70
CHEMBL4553794 IC50 = 2000.0 nM 5.70
CHEMBL5743998 IC50 = 2000.0 nM 5.70
CHEMBL6039146 IC50 = 2000.0 nM 5.70
CHEMBL5956917 IC50 = 2000.0 nM 5.70
CHEMBL5929671 IC50 = 2000.0 nM 5.70
CHEMBL6057874 IC50 = 2000.0 nM 5.70
CHEMBL6012461 IC50 = 2000.0 nM 5.70
CHEMBL5819053 IC50 = 2000.0 nM 5.70
CHEMBL6027891 IC50 = 2000.0 nM 5.70
CHEMBL6009962 IC50 = 2000.0 nM 5.70
CHEMBL5869739 IC50 = 2000.0 nM 5.70
CHEMBL5929479 IC50 = 2000.0 nM 5.70
CHEMBL5902643 IC50 = 2000.0 nM 5.70
CHEMBL4573202 IC50 = 2000.0 nM 5.70
CHEMBL6035831 IC50 = 2000.0 nM 5.70
CHEMBL5836988 IC50 = 2000.0 nM 5.70
CHEMBL5936717 IC50 = 2000.0 nM 5.70
CHEMBL5875670 IC50 = 2000.0 nM 5.70
CHEMBL5835884 IC50 = 3000.0 nM 5.52
CHEMBL4457401 IC50 = 3000.0 nM 5.52
CHEMBL5858329 IC50 = 3000.0 nM 5.52
CHEMBL5893609 IC50 = 3000.0 nM 5.52