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Assay Detail

CHEMBL615539

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Functional
Inhibition of forskolin-stimulated lipolysis in differentiated 3T3-L1 cells
ChEMBL ↗
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type 3T3-L1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Hormone-sensitive lipase (CHEMBL3590) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

In vitro SAR of (5-(2H)-isoxazolonyl) ureas, potent inhibitors of hormone-sensitive lipase.
Lowe DB, Magnuson S, Qi N, Campbell AM, Cook J, Hong Z, Wang M, Rodriguez M, Achebe F, Kluender H, Wong WC, Bullock WH, Salhanick AI, Witman-Jones T, Bowling ME, Keiper C, Clairmont KB.
Bioorg Med Chem Lett (2004) 14 : 3155 -3159
PubMed 15149665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 72 7.25 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106375 — — 1 9.70
CHEMBL110343 — — 1 8.70
CHEMBL107197 — — 1 8.52
CHEMBL106784 — — 1 8.40
CHEMBL317407 — — 1 8.40
CHEMBL108523 — — 1 8.40
CHEMBL320249 — — 1 8.30
CHEMBL320708 — — 1 8.10
CHEMBL106756 — — 1 8.05
CHEMBL322794 — — 1 8.00
CHEMBL105834 — — 1 8.00
CHEMBL107365 — — 1 7.92
CHEMBL419197 — — 1 7.89
CHEMBL106581 — — 1 7.75
CHEMBL110763 — — 1 7.70
CHEMBL320813 — — 1 7.70
CHEMBL321903 — — 1 7.66
CHEMBL108325 — — 1 7.62
CHEMBL323458 — — 1 7.57
CHEMBL110655 — — 1 7.57
CHEMBL106126 — — 1 7.55
CHEMBL320525 — — 1 7.55
CHEMBL321433 — — 1 7.51
CHEMBL110653 — — 1 7.50
CHEMBL106504 — — 1 7.48
CHEMBL108519 — — 1 7.40
CHEMBL321483 — — 1 7.32
CHEMBL110716 — — 1 7.31
CHEMBL110166 — — 1 7.29
CHEMBL108568 — — 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106375 — IC50 = 0.2 nM 9.70
CHEMBL110343 — IC50 = 2.0 nM 8.70
CHEMBL107197 — IC50 = 3.0 nM 8.52
CHEMBL106784 — IC50 = 4.0 nM 8.40
CHEMBL317407 — IC50 = 4.0 nM 8.40
CHEMBL108523 — IC50 = 4.0 nM 8.40
CHEMBL320249 — IC50 = 5.0 nM 8.30
CHEMBL320708 — IC50 = 8.0 nM 8.10
CHEMBL106756 — IC50 = 9.0 nM 8.05
CHEMBL322794 — IC50 = 10.0 nM 8.00
CHEMBL105834 — IC50 = 10.0 nM 8.00
CHEMBL107365 — IC50 = 12.0 nM 7.92
CHEMBL419197 — IC50 = 13.0 nM 7.89
CHEMBL106581 — IC50 = 18.0 nM 7.75
CHEMBL320813 — IC50 = 20.0 nM 7.70
CHEMBL110763 — IC50 = 20.0 nM 7.70
CHEMBL321903 — IC50 = 22.0 nM 7.66
CHEMBL108325 — IC50 = 24.0 nM 7.62
CHEMBL323458 — IC50 = 27.0 nM 7.57
CHEMBL110655 — IC50 = 27.0 nM 7.57
CHEMBL106126 — IC50 = 28.0 nM 7.55
CHEMBL320525 — IC50 = 28.0 nM 7.55
CHEMBL321433 — IC50 = 31.0 nM 7.51
CHEMBL110653 — IC50 = 32.0 nM 7.50
CHEMBL106504 — IC50 = 33.0 nM 7.48
CHEMBL108519 — IC50 = 40.0 nM 7.40
CHEMBL321483 — IC50 = 48.0 nM 7.32
CHEMBL110716 — IC50 = 49.0 nM 7.31
CHEMBL110166 — IC50 = 51.0 nM 7.29
CHEMBL108568 — IC50 = 56.0 nM 7.25
CHEMBL108207 — IC50 = 61.0 nM 7.21
CHEMBL106314 — IC50 = 67.0 nM 7.17
CHEMBL106987 — IC50 = 73.0 nM 7.14
CHEMBL109116 — IC50 = 75.0 nM 7.12
CHEMBL106045 — IC50 = 90.0 nM 7.05
CHEMBL110322 — IC50 = 90.0 nM 7.05
CHEMBL323419 — IC50 = 98.0 nM 7.01
CHEMBL325369 — IC50 = 120.0 nM 6.92
CHEMBL316549 — IC50 = 135.0 nM 6.87
CHEMBL110731 — IC50 = 140.0 nM 6.85
CHEMBL110717 — IC50 = 150.0 nM 6.82
CHEMBL107712 — IC50 = 150.0 nM 6.82
CHEMBL317643 — IC50 = 170.0 nM 6.77
CHEMBL109182 — IC50 = 180.0 nM 6.75
CHEMBL323173 — IC50 = 177.0 nM 6.75
CHEMBL108270 — IC50 = 187.0 nM 6.73
CHEMBL106200 — IC50 = 190.0 nM 6.72
CHEMBL110597 — IC50 = 190.0 nM 6.72
CHEMBL106503 — IC50 = 200.0 nM 6.70
CHEMBL106729 — IC50 = 215.0 nM 6.67