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Assay Detail

CHEMBL4703203

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Binding
Inhibition of recombinant human sEH expressed in baculovirus expression system assessed as reduction in ACPU binding incubated for 1 hr by FRET displacement assay
ChEMBL ↗
46
Total Activities
46
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

Bifunctional epoxide hydrolase 2 (CHEMBL2409) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preparation and evaluation of soluble epoxide hydrolase inhibitors with improved physical properties and potencies for treating diabetic neuropathic pain.
Lee KSS,Ng JC,Yang J,Hwang SH,Morisseau C,Wagner K,Hammock BD
Bioorg Med Chem (2020) 28 : 115735 -115735
PubMed 33007552 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 46 8.95 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4752831 — — 1 10.10
CHEMBL4748112 — — 1 9.82
CHEMBL4781745 — — 1 9.66
CHEMBL3327067 — — 1 9.66
CHEMBL4764213 — — 1 9.59
CHEMBL4743434 — — 1 9.51
CHEMBL4752121 — — 1 9.48
CHEMBL4741174 — — 1 9.43
CHEMBL4780369 — — 1 9.42
CHEMBL4756077 — — 1 9.42
CHEMBL4749102 — — 1 9.31
CHEMBL4749079 — — 1 9.30
CHEMBL4740401 — — 1 9.29
CHEMBL4743354 — — 1 9.26
CHEMBL4740980 — — 1 9.19
CHEMBL4742765 — — 1 9.15
CHEMBL4764831 — — 1 9.15
CHEMBL4776917 — — 1 9.12
CHEMBL4756688 — — 1 9.11
CHEMBL4782162 — — 1 9.11
CHEMBL4749869 — — 1 9.06
CHEMBL4796253 — — 1 8.99
CHEMBL4760004 — — 1 8.92
CHEMBL4746684 — — 1 8.92
CHEMBL4744784 — — 1 8.85
CHEMBL4750425 — — 1 8.85
CHEMBL4763353 — — 1 8.77
CHEMBL4780067 — — 1 8.76
CHEMBL4800691 — — 1 8.76
CHEMBL4799231 — — 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4752831 — Ki = 0.08 nM 10.10
CHEMBL4748112 — Ki = 0.15 nM 9.82
CHEMBL3327067 — Ki = 0.22 nM 9.66
CHEMBL4781745 — Ki = 0.22 nM 9.66
CHEMBL4764213 — Ki = 0.26 nM 9.59
CHEMBL4743434 — Ki = 0.31 nM 9.51
CHEMBL4752121 — Ki = 0.33 nM 9.48
CHEMBL4741174 — Ki = 0.37 nM 9.43
CHEMBL4780369 — Ki = 0.38 nM 9.42
CHEMBL4756077 — Ki = 0.38 nM 9.42
CHEMBL4749102 — Ki = 0.49 nM 9.31
CHEMBL4749079 — Ki = 0.5 nM 9.30
CHEMBL4740401 — Ki = 0.51 nM 9.29
CHEMBL4743354 — Ki = 0.55 nM 9.26
CHEMBL4740980 — Ki = 0.64 nM 9.19
CHEMBL4742765 — Ki = 0.7 nM 9.15
CHEMBL4764831 — Ki = 0.7 nM 9.15
CHEMBL4776917 — Ki = 0.75 nM 9.12
CHEMBL4756688 — Ki = 0.77 nM 9.11
CHEMBL4782162 — Ki = 0.78 nM 9.11
CHEMBL4749869 — Ki = 0.87 nM 9.06
CHEMBL4796253 — Ki = 1.03 nM 8.99
CHEMBL4746684 — Ki = 1.19 nM 8.92
CHEMBL4760004 — Ki = 1.21 nM 8.92
CHEMBL4744784 — Ki = 1.43 nM 8.85
CHEMBL4750425 — Ki = 1.41 nM 8.85
CHEMBL4763353 — Ki = 1.7 nM 8.77
CHEMBL4780067 — Ki = 1.74 nM 8.76
CHEMBL4800691 — Ki = 1.73 nM 8.76
CHEMBL4799231 — Ki = 1.99 nM 8.70
CHEMBL4750293 — Ki = 2.09 nM 8.68
CHEMBL4791464 — Ki = 2.4 nM 8.62
CHEMBL4790379 — Ki = 2.66 nM 8.57
CHEMBL4795460 — Ki = 2.94 nM 8.53
CHEMBL4763290 — Ki = 3.14 nM 8.50
CHEMBL4799241 — Ki = 3.35 nM 8.47
CHEMBL4763640 — Ki = 3.4 nM 8.47
CHEMBL4777697 — Ki = 3.83 nM 8.42
CHEMBL4797107 — Ki = 4.72 nM 8.33
CHEMBL4781646 — Ki = 6.6 nM 8.18
CHEMBL4747426 — Ki = 9.07 nM 8.04
CHEMBL4760255 — Ki = 9.91 nM 8.00
CHEMBL4761917 — Ki = 45.0 nM 7.35
CHEMBL4752759 — Ki < 0.05 nM -
CHEMBL4756603 — Ki < 0.05 nM -
CHEMBL4789214 — Ki < 0.05 nM -