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Assay Detail

CHEMBL5734306

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Binding
Inhibition Assay: The enzyme also can be detected based on the binding of specific ligands to the catalytic site which either immobilize the enzyme or label it with a probe such as dansyl, fluoracein, luciferase, green fluorescent protein or other reagent. The enzyme can be assayed by its hydration of EETs, its hydrolysis of an epoxide to give a colored product. The assays are normally carried out with a recombinant enzyme following affinity purification.
48
Total Activities
15
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Treatment of inflammatory disorders in non-human mammals
(2019)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.19 9.00
kon 16 - -
k_off 16 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6041919 6 9.00
CHEMBL6027597 3 9.00
CHEMBL3901070 3 9.00
CHEMBL3895613 3 9.00
CHEMBL1766285 3 8.70
CHEMBL215387 3 8.52
CHEMBL242655 3 8.52
CHEMBL5943959 3 8.30
CHEMBL1257405 3 7.75
CHEMBL1257634 3 7.52
CHEMBL1257635 3 7.48
CHEMBL1258904 3 7.36
CHEMBL1076347 TRICLOCARBAN 2.0 3 7.25
CHEMBL436774 AR9281 2.0 3 7.17
CHEMBL1668934 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6041919 IC50 = 1.0 nM 9.00
CHEMBL3895613 IC50 = 1.0 nM 9.00
CHEMBL3901070 IC50 = 1.0 nM 9.00
CHEMBL6027597 IC50 = 1.0 nM 9.00
CHEMBL1766285 IC50 = 2.0 nM 8.70
CHEMBL215387 IC50 = 3.0 nM 8.52
CHEMBL242655 IC50 = 3.0 nM 8.52
CHEMBL5943959 IC50 = 5.0 nM 8.30
CHEMBL6041919 IC50 = 6.0 nM 8.22
CHEMBL1257405 IC50 = 18.0 nM 7.75
CHEMBL1257634 IC50 = 30.0 nM 7.52
CHEMBL1257635 IC50 = 33.0 nM 7.48
CHEMBL1258904 IC50 = 44.0 nM 7.36
CHEMBL1076347 TRICLOCARBAN IC50 = 56.0 nM 7.25
CHEMBL436774 AR9281 IC50 = 67.0 nM 7.17
CHEMBL215387 k_off = - s-1 -
CHEMBL242655 kon = - -
CHEMBL242655 k_off = - s-1 -
CHEMBL436774 AR9281 kon = - -
CHEMBL436774 AR9281 k_off = - s-1 -
CHEMBL5943959 kon = - -
CHEMBL1258904 kon = - -
CHEMBL1668934 IC50 > 10000.0 nM -
CHEMBL1668934 kon = - -
CHEMBL1668934 k_off = - s-1 -
CHEMBL6041919 kon = - -
CHEMBL6041919 k_off = - s-1 -
CHEMBL1257634 kon = - -
CHEMBL1257634 k_off = - s-1 -
CHEMBL6041919 kon = - -
CHEMBL6041919 k_off = - s-1 -
CHEMBL1257635 kon = - -
CHEMBL6027597 k_off = - s-1 -
CHEMBL6027597 kon = - -
CHEMBL3901070 kon = - -
CHEMBL1257405 k_off = - s-1 -
CHEMBL3901070 k_off = - s-1 -
CHEMBL1257405 kon = - -
CHEMBL3895613 kon = - -
CHEMBL1257635 k_off = - s-1 -
CHEMBL215387 kon = - -
CHEMBL3895613 k_off = - s-1 -
CHEMBL1766285 kon = - -
CHEMBL1258904 k_off = - s-1 -
CHEMBL1766285 k_off = - s-1 -
CHEMBL5943959 k_off = - s-1 -
CHEMBL1076347 TRICLOCARBAN kon = - -
CHEMBL1076347 TRICLOCARBAN k_off = - s-1 -