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Assay Detail

CHEMBL3116602

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

Binding
Inhibition of N-terminal His6-tagged human platelet 12-LOX using arachidonic acid as substrate by UV-vis spectrophotometric analysis
ChEMBL ↗
74
Total Activities
74
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

Polyunsaturated fatty acid lipoxygenase ALOX12 (CHEMBL3687) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase.
Luci DK, Jameson JB, Yasgar A, Diaz G, Joshi N, Kantz A, Markham K, Perry S, Kuhn N, Yeung J, Kerns EH, Schultz L, Holinstat M, Nadler JL, Taylor-Fishwick DA, Jadhav A, Simeonov A, Holman TR, Maloney DJ.
J Med Chem (2014) 57 : 495 -506
PubMed 24393039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 74 5.71 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3113197 — — 1 6.80
CHEMBL3113193 — — 1 6.75
CHEMBL3113198 — — 1 6.66
CHEMBL3113169 — — 1 6.62
CHEMBL3113192 — — 1 6.58
CHEMBL3113180 — — 1 6.48
CHEMBL3113165 VLX-1005 2.0 1 6.47
CHEMBL3113168 — — 1 6.46
CHEMBL3113191 — — 1 6.41
CHEMBL3113176 — — 1 6.32
CHEMBL3113178 — — 1 6.30
CHEMBL3113179 — — 1 6.29
CHEMBL3113167 — — 1 6.24
CHEMBL3113177 — — 1 6.16
CHEMBL3113195 — — 1 6.12
CHEMBL3113166 — — 1 6.10
CHEMBL3113196 — — 1 5.96
CHEMBL3113201 — — 1 5.89
CHEMBL3113181 — — 1 5.89
CHEMBL3113369 — — 1 5.89
CHEMBL3113173 — — 1 5.85
CHEMBL3113200 — — 1 5.80
CHEMBL3113370 — — 1 5.77
CHEMBL3113152 — — 1 5.66
CHEMBL3113372 — — 1 5.66
CHEMBL3113371 — — 1 5.64
CHEMBL3113202 — — 1 5.64
CHEMBL3113373 — — 1 5.60
CHEMBL3113170 — — 1 5.57
CHEMBL3113368 — — 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3113197 — IC50 = 160.0 nM 6.80
CHEMBL3113193 — IC50 = 180.0 nM 6.75
CHEMBL3113198 — IC50 = 220.0 nM 6.66
CHEMBL3113169 — IC50 = 240.0 nM 6.62
CHEMBL3113192 — IC50 = 260.0 nM 6.58
CHEMBL3113180 — IC50 = 330.0 nM 6.48
CHEMBL3113165 VLX-1005 IC50 = 340.0 nM 6.47
CHEMBL3113168 — IC50 = 350.0 nM 6.46
CHEMBL3113191 — IC50 = 390.0 nM 6.41
CHEMBL3113176 — IC50 = 480.0 nM 6.32
CHEMBL3113178 — IC50 = 500.0 nM 6.30
CHEMBL3113179 — IC50 = 510.0 nM 6.29
CHEMBL3113167 — IC50 = 570.0 nM 6.24
CHEMBL3113177 — IC50 = 700.0 nM 6.16
CHEMBL3113195 — IC50 = 760.0 nM 6.12
CHEMBL3113166 — IC50 = 790.0 nM 6.10
CHEMBL3113196 — IC50 = 1100.0 nM 5.96
CHEMBL3113201 — IC50 = 1300.0 nM 5.89
CHEMBL3113181 — IC50 = 1300.0 nM 5.89
CHEMBL3113369 — IC50 = 1300.0 nM 5.89
CHEMBL3113173 — IC50 = 1400.0 nM 5.85
CHEMBL3113200 — IC50 = 1600.0 nM 5.80
CHEMBL3113370 — IC50 = 1700.0 nM 5.77
CHEMBL3113152 — IC50 = 2200.0 nM 5.66
CHEMBL3113372 — IC50 = 2200.0 nM 5.66
CHEMBL3113371 — IC50 = 2300.0 nM 5.64
CHEMBL3113202 — IC50 = 2300.0 nM 5.64
CHEMBL3113373 — IC50 = 2500.0 nM 5.60
CHEMBL3113170 — IC50 = 2700.0 nM 5.57
CHEMBL3113368 — IC50 = 2900.0 nM 5.54
CHEMBL3113171 — IC50 = 3000.0 nM 5.52
CHEMBL3113183 — IC50 = 3500.0 nM 5.46
CHEMBL3113185 — IC50 = 3700.0 nM 5.43
CHEMBL3113194 — IC50 = 3800.0 nM 5.42
CHEMBL3113186 — IC50 = 4000.0 nM 5.40
CHEMBL3113203 — IC50 = 4200.0 nM 5.38
CHEMBL3113199 — IC50 = 4500.0 nM 5.35
CHEMBL3113204 — IC50 = 4500.0 nM 5.35
CHEMBL3113187 — IC50 = 5000.0 nM 5.30
CHEMBL3113188 — IC50 = 5000.0 nM 5.30
CHEMBL1596118 — IC50 = 5100.0 nM 5.29
CHEMBL3113366 — IC50 = 5300.0 nM 5.28
CHEMBL3113374 — IC50 = 5600.0 nM 5.25
CHEMBL3113386 — IC50 = 6200.0 nM 5.21
CHEMBL3113367 — IC50 = 6300.0 nM 5.20
CHEMBL3113157 — IC50 = 6300.0 nM 5.20
CHEMBL3113189 — IC50 = 7000.0 nM 5.16
CHEMBL3113184 — IC50 = 11000.0 nM 4.96
CHEMBL3113174 — IC50 = 11000.0 nM 4.96
CHEMBL3113190 — IC50 = 12000.0 nM 4.92