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Assay Detail

CHEMBL619950

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

Binding
In vitro inhibitory activity against 5-lipoxygenase from rat basophilic leukemia cells.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and 5-lipoxygenase inhibitory activity of 5-hydroperoxy-6,8,11,14-eicosatetraenoic acid analogues.
Kerdesky FA, Schmidt SP, Holms JH, Dyer RD, Carter GW, Brooks DW.
J Med Chem (1987) 30 : 1177 -1186
PubMed 3599023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 4.93 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL557132 1 6.72
CHEMBL274642 BW-755C 1 5.89
CHEMBL18178 1 5.85
CHEMBL18129 1 5.68
CHEMBL7660 PHENIDONE 1 5.68
CHEMBL277123 1 5.66
CHEMBL17757 1 5.55
CHEMBL18201 1 5.16
CHEMBL18221 1 5.14
CHEMBL18117 1 5.12
CHEMBL429224 1 5.10
CHEMBL17922 1 5.00
CHEMBL18054 1 4.96
CHEMBL18379 1 4.96
CHEMBL18028 5-OXO-ETE 1 4.75
CHEMBL17883 1 4.68
CHEMBL18112 1 4.66
CHEMBL263073 1 4.60
CHEMBL18584 1 4.60
CHEMBL276929 1 4.57
CHEMBL17775 1 4.54
CHEMBL418364 1 4.44
CHEMBL277539 1 4.26
CHEMBL17983 1 4.23
CHEMBL275848 1 4.17
CHEMBL17695 1 4.11
CHEMBL18239 1 4.02
CHEMBL18435 1 4.01
CHEMBL8747 REV-5901 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL557132 IC50 = 190.0 nM 6.72
CHEMBL274642 BW-755C IC50 = 1300.0 nM 5.89
CHEMBL18178 IC50 = 1400.0 nM 5.85
CHEMBL18129 IC50 = 2100.0 nM 5.68
CHEMBL7660 PHENIDONE IC50 = 2100.0 nM 5.68
CHEMBL277123 IC50 = 2200.0 nM 5.66
CHEMBL17757 IC50 = 2800.0 nM 5.55
CHEMBL18201 IC50 = 7000.0 nM 5.16
CHEMBL18221 IC50 = 7300.0 nM 5.14
CHEMBL18117 IC50 = 7600.0 nM 5.12
CHEMBL429224 IC50 = 7900.0 nM 5.10
CHEMBL17922 IC50 = 10000.0 nM 5.00
CHEMBL18054 IC50 = 11000.0 nM 4.96
CHEMBL18379 IC50 = 11000.0 nM 4.96
CHEMBL18028 5-OXO-ETE IC50 = 18000.0 nM 4.75
CHEMBL17883 IC50 = 21000.0 nM 4.68
CHEMBL18112 IC50 = 22000.0 nM 4.66
CHEMBL263073 IC50 = 25000.0 nM 4.60
CHEMBL18584 IC50 = 25000.0 nM 4.60
CHEMBL276929 IC50 = 27000.0 nM 4.57
CHEMBL17775 IC50 = 29000.0 nM 4.54
CHEMBL418364 IC50 = 36000.0 nM 4.44
CHEMBL277539 IC50 = 55000.0 nM 4.26
CHEMBL17983 IC50 = 59000.0 nM 4.23
CHEMBL275848 IC50 = 68000.0 nM 4.17
CHEMBL17695 IC50 = 77000.0 nM 4.11
CHEMBL18239 IC50 = 96000.0 nM 4.02
CHEMBL18435 IC50 = 97000.0 nM 4.01
CHEMBL8747 REV-5901 IC50 > 45000.0 nM -