Assay Detail

CHEMBL4839666

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Binding

Inhibition of human 12-LOX A417I/V418M double mutant using arachidonic acid as substrate by UV-Vis spectroscopy analysis

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Docking and mutagenesis studies lead to improved inhibitor development of ML355 for human platelet 12-lipoxygenase.

Tsai WC, Aleem AM, Tena J, Rivera-Velazquez M, Brah HS, Tripathi S, D'silva M, Nadler JL, Kalyanaraman C, Jacobson MP, Holman T.
Bioorg Med Chem (2021) 46 : 116347 -116347
PubMed 34507163 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	6.50	6.92

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4869861	—	—	1	6.92
CHEMBL3113165	VLX-1005	2.0	1	6.08

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4869861	—	IC50	=	120.0	nM	6.92
CHEMBL3113165	VLX-1005	IC50	=	830.0	nM	6.08