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Assay Detail

CHEMBL3118263

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Binding
Inhibition of rat recombinant soluble epoxide hydrolase after 1 hr by fluorescence assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bifunctional epoxide hydrolase 2 (CHEMBL5669)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-based optimization of cyclopropyl urea derivatives as potent soluble epoxide hydrolase inhibitors for potential decrease of renal injury without hypotensive action.
Takai K, Nakajima T, Takanashi Y, Sone T, Nariai T, Chiyo N, Nakatani S, Ishikawa C, Yamaguchi N, Fujita K, Yamada K.
Bioorg Med Chem (2014) 22 : 1548 -1557
PubMed 24530032 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 8.02 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3114595 1 8.49
CHEMBL3114618 1 8.46
CHEMBL3114609 1 8.39
CHEMBL3114592 1 8.38
CHEMBL3114600 1 8.30
CHEMBL3114599 1 8.29
CHEMBL3114617 1 8.28
CHEMBL3114602 1 8.23
CHEMBL3114593 1 8.19
CHEMBL3114610 1 8.18
CHEMBL3114608 1 8.18
CHEMBL3114603 1 8.17
CHEMBL3114594 1 8.17
CHEMBL3114590 1 8.10
CHEMBL1615216 1 8.08
CHEMBL3114597 1 8.05
CHEMBL3114591 1 8.03
CHEMBL3114596 1 7.98
CHEMBL3114614 1 7.91
CHEMBL3114598 1 7.89
CHEMBL3114611 1 7.74
CHEMBL3114613 1 7.70
CHEMBL3114601 1 7.68
CHEMBL3114616 1 7.59
CHEMBL3114606 1 7.49
CHEMBL3114612 1 7.45
CHEMBL3114607 1 7.25
CHEMBL3114604 1 -
CHEMBL3114605 1 -
CHEMBL3114615 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3114595 IC50 = 3.2 nM 8.49
CHEMBL3114618 IC50 = 3.5 nM 8.46
CHEMBL3114609 IC50 = 4.1 nM 8.39
CHEMBL3114592 IC50 = 4.2 nM 8.38
CHEMBL3114600 IC50 = 5.0 nM 8.30
CHEMBL3114599 IC50 = 5.1 nM 8.29
CHEMBL3114617 IC50 = 5.2 nM 8.28
CHEMBL3114602 IC50 = 5.9 nM 8.23
CHEMBL3114593 IC50 = 6.5 nM 8.19
CHEMBL3114610 IC50 = 6.6 nM 8.18
CHEMBL3114608 IC50 = 6.6 nM 8.18
CHEMBL3114603 IC50 = 6.7 nM 8.17
CHEMBL3114594 IC50 = 6.8 nM 8.17
CHEMBL3114590 IC50 = 8.0 nM 8.10
CHEMBL1615216 IC50 = 8.3 nM 8.08
CHEMBL3114597 IC50 = 8.9 nM 8.05
CHEMBL3114591 IC50 = 9.3 nM 8.03
CHEMBL3114596 IC50 = 10.5 nM 7.98
CHEMBL3114614 IC50 = 12.3 nM 7.91
CHEMBL3114598 IC50 = 12.8 nM 7.89
CHEMBL3114611 IC50 = 18.3 nM 7.74
CHEMBL3114613 IC50 = 20.2 nM 7.70
CHEMBL3114601 IC50 = 20.7 nM 7.68
CHEMBL3114616 IC50 = 25.6 nM 7.59
CHEMBL3114606 IC50 = 32.2 nM 7.49
CHEMBL3114612 IC50 = 35.4 nM 7.45
CHEMBL3114607 IC50 = 56.6 nM 7.25
CHEMBL3114604 IC50 > 100.0 nM -
CHEMBL3114605 IC50 > 100.0 nM -
CHEMBL3114615 IC50 > 100.0 nM -