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Assay Detail

CHEMBL3756328

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Binding
Inhibition of full-length human DAGLalpha expressed in HEK293T cell membranes using para-nitrophenylbutyrate by colorimetric assay
ChEMBL ↗
124
Total Activities
123
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Diacylglycerol lipase-alpha (CHEMBL5545) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Comprehensive Analysis of Structure-Activity Relationships of α-Ketoheterocycles as sn-1-Diacylglycerol Lipase α Inhibitors.
Janssen FJ, Baggelaar MP, Hummel JJ, Overkleeft HS, Cravatt BF, Boger DL, van der Stelt M.
J Med Chem (2015) 58 : 9742 -9753
PubMed 26584396 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 123 6.25 8.44
pIC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182199 — — 1 8.44
CHEMBL35925 — — 1 7.58
CHEMBL257307 — — 1 7.51
CHEMBL175854 — — 1 7.43
CHEMBL179760 — — 1 7.33
CHEMBL1812706 — — 1 7.19
CHEMBL1812708 — — 1 7.13
CHEMBL1812707 — — 1 7.13
CHEMBL3753830 — — 1 7.06
CHEMBL3754098 — — 1 6.93
CHEMBL461543 — — 1 6.91
CHEMBL461364 — — 1 6.91
CHEMBL3753992 — — 1 6.71
CHEMBL464186 — — 1 6.69
CHEMBL3753016 — — 1 6.69
CHEMBL461544 — — 1 6.67
CHEMBL3753217 — — 1 6.41
CHEMBL3752580 — — 1 6.32
CHEMBL367966 — — 1 6.28
CHEMBL3754151 — — 1 6.26
CHEMBL462423 — — 1 6.24
CHEMBL257305 — — 1 6.20
CHEMBL461539 — — 1 6.20
CHEMBL3753292 — — 1 6.15
CHEMBL3753795 — — 1 6.05
CHEMBL469199 — — 1 6.03
CHEMBL469241 — — 1 5.98
CHEMBL3753568 — — 1 5.91
CHEMBL3752691 — — 1 5.85
CHEMBL461315 — — 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182199 — IC50 = 3.631 nM 8.44
CHEMBL35925 — IC50 = 26.3 nM 7.58
CHEMBL257307 — IC50 = 30.9 nM 7.51
CHEMBL175854 — IC50 = 37.15 nM 7.43
CHEMBL179760 — IC50 = 46.77 nM 7.33
CHEMBL1812706 — IC50 = 64.57 nM 7.19
CHEMBL1812708 — IC50 = 74.13 nM 7.13
CHEMBL1812707 — IC50 = 74.13 nM 7.13
CHEMBL3753830 — IC50 = 87.1 nM 7.06
CHEMBL3754098 — IC50 = 117.49 nM 6.93
CHEMBL461364 — IC50 = 123.03 nM 6.91
CHEMBL461543 — IC50 = 123.03 nM 6.91
CHEMBL3753992 — IC50 = 194.98 nM 6.71
CHEMBL464186 — IC50 = 204.17 nM 6.69
CHEMBL3753016 — IC50 = 204.17 nM 6.69
CHEMBL461544 — IC50 = 213.8 nM 6.67
CHEMBL3753217 — IC50 = 389.05 nM 6.41
CHEMBL3752580 — IC50 = 478.63 nM 6.32
CHEMBL367966 — IC50 = 524.81 nM 6.28
CHEMBL3754151 — IC50 = 549.54 nM 6.26
CHEMBL462423 — IC50 = 575.44 nM 6.24
CHEMBL257305 — IC50 = 630.96 nM 6.20
CHEMBL461539 — IC50 = 630.96 nM 6.20
CHEMBL3753292 — IC50 = 707.95 nM 6.15
CHEMBL3753795 — IC50 = 891.25 nM 6.05
CHEMBL469199 — IC50 = 933.25 nM 6.03
CHEMBL469241 — IC50 = 1047.13 nM 5.98
CHEMBL3753568 — IC50 = 1230.27 nM 5.91
CHEMBL3752691 — IC50 = 1412.54 nM 5.85
CHEMBL461315 — IC50 = 1513.56 nM 5.82
CHEMBL3752838 — IC50 = 1698.24 nM 5.77
CHEMBL220378 — IC50 = 1819.7 nM 5.74
CHEMBL466954 — IC50 = 1949.84 nM 5.71
CHEMBL513534 — IC50 = 2041.74 nM 5.69
CHEMBL257638 — IC50 = 2238.72 nM 5.65
CHEMBL462302 — IC50 = 2344.23 nM 5.63
CHEMBL371831 — IC50 = 2398.83 nM 5.62
CHEMBL462432 — IC50 = 2398.83 nM 5.62
CHEMBL467796 — IC50 = 2691.53 nM 5.57
CHEMBL469198 — IC50 = 2754.23 nM 5.56
CHEMBL462589 — IC50 = 3388.44 nM 5.47
CHEMBL366907 — IC50 = 3630.78 nM 5.44
CHEMBL3754118 — IC50 = 5888.44 nM 5.23
CHEMBL460316 — IC50 = 8709.64 nM 5.06
CHEMBL3752944 — IC50 = 12022.64 nM 4.92
CHEMBL3754440 — IC50 = 18197.01 nM 4.74
CHEMBL467141 — IC50 > 10000.0 nM -
CHEMBL468585 — IC50 > 10000.0 nM -
CHEMBL469252 — IC50 > 10000.0 nM -
CHEMBL467368 — IC50 > 10000.0 nM -