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Assay Detail

CHEMBL3608050

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

Binding
Inhibition of human 15-LOX-1 expressed in Sf9 cells assessed as reduction in conversion of arachidonic acid to 15-HETE pre-incubated 5 min before arachidonic acid substrate addition by HPLC-UV spectroscopy
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Polyunsaturated fatty acid lipoxygenase ALOX15 (CHEMBL2903)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1.
Pelcman B, Sanin A, Nilsson P, No K, Schaal W, Öhrman S, Krog-Jensen C, Forsell P, Hallberg A, Larhed M, Boesen T, Kromann H, Vogensen SB, Groth T, Claesson HE.
Bioorg Med Chem Lett (2015) 25 : 3024 -3029
PubMed 26037322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 6.51 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3604156 1 9.00
CHEMBL3604185 1 8.70
CHEMBL3604184 1 8.40
CHEMBL3604180 1 7.70
CHEMBL3604138 1 7.58
CHEMBL3604153 1 7.50
CHEMBL3604152 1 7.15
CHEMBL3604132 1 7.09
CHEMBL3604151 1 7.07
CHEMBL3604174 1 7.00
CHEMBL3604158 1 6.82
CHEMBL3604134 1 6.78
CHEMBL3604141 1 6.75
CHEMBL3604131 1 6.75
CHEMBL3604157 1 6.74
CHEMBL3604155 1 6.54
CHEMBL3604140 1 6.48
CHEMBL3604139 1 6.42
CHEMBL3604147 1 6.42
CHEMBL3604181 1 6.35
CHEMBL3604133 1 6.35
CHEMBL3604146 1 6.34
CHEMBL3604137 1 6.26
CHEMBL3604173 1 6.24
CHEMBL3604166 1 6.19
CHEMBL1587607 1 6.19
CHEMBL3604145 1 6.17
CHEMBL3604143 1 6.07
CHEMBL3604171 1 6.02
CHEMBL3604142 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3604156 IC50 = 1.0 nM 9.00
CHEMBL3604185 IC50 = 2.0 nM 8.70
CHEMBL3604184 IC50 = 4.0 nM 8.40
CHEMBL3604180 IC50 = 20.0 nM 7.70
CHEMBL3604138 IC50 = 26.0 nM 7.58
CHEMBL3604153 IC50 = 32.0 nM 7.50
CHEMBL3604152 IC50 = 71.0 nM 7.15
CHEMBL3604132 IC50 = 81.0 nM 7.09
CHEMBL3604151 IC50 = 85.0 nM 7.07
CHEMBL3604174 IC50 = 99.0 nM 7.00
CHEMBL3604158 IC50 = 150.0 nM 6.82
CHEMBL3604134 IC50 = 168.0 nM 6.78
CHEMBL3604131 IC50 = 180.0 nM 6.75
CHEMBL3604141 IC50 = 180.0 nM 6.75
CHEMBL3604157 IC50 = 184.0 nM 6.74
CHEMBL3604155 IC50 = 290.0 nM 6.54
CHEMBL3604140 IC50 = 334.0 nM 6.48
CHEMBL3604139 IC50 = 384.0 nM 6.42
CHEMBL3604147 IC50 = 376.0 nM 6.42
CHEMBL3604181 IC50 = 443.0 nM 6.35
CHEMBL3604133 IC50 = 448.0 nM 6.35
CHEMBL3604146 IC50 = 453.0 nM 6.34
CHEMBL3604137 IC50 = 550.0 nM 6.26
CHEMBL3604173 IC50 = 571.0 nM 6.24
CHEMBL1587607 IC50 = 645.0 nM 6.19
CHEMBL3604166 IC50 = 641.0 nM 6.19
CHEMBL3604145 IC50 = 672.0 nM 6.17
CHEMBL3604143 IC50 = 843.0 nM 6.07
CHEMBL3604171 IC50 = 947.0 nM 6.02
CHEMBL3604142 IC50 = 970.0 nM 6.01
CHEMBL3604160 IC50 = 1000.0 nM 6.00
CHEMBL3604135 IC50 = 1207.0 nM 5.92
CHEMBL3604177 IC50 = 1400.0 nM 5.85
CHEMBL3604179 IC50 = 3273.0 nM 5.49
CHEMBL3604176 IC50 = 3965.0 nM 5.40
CHEMBL3603844 IC50 = 5900.0 nM 5.23
CHEMBL3604167 IC50 = 5980.0 nM 5.22
CHEMBL3604172 IC50 = 6976.0 nM 5.16
CHEMBL3604175 IC50 = 22530.0 nM 4.65
CHEMBL3604136 IC50 - -
CHEMBL3604170 IC50 - -
CHEMBL3604178 IC50 - -
CHEMBL3604182 IC50 - -
CHEMBL3604183 IC50 - -
CHEMBL3604154 IC50 - -
CHEMBL3604150 IC50 - -
CHEMBL3604149 IC50 - -
CHEMBL3604148 IC50 - -
CHEMBL3604144 IC50 - -
CHEMBL3604129 IC50 - -