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Assay Detail

CHEMBL4392491

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Binding
Inhibition of mouse DGAT1
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Diacylglycerol O-acyltransferase 1 (CHEMBL1075284)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).
Yu Y, Wu Z, Shi ZC, He S, Lai Z, Cernak TA, Vachal P, Liu M, Liu J, Hong Q, Jian T, Guiadeen D, Krikorian A, Sperbeck DM, Verras A, Sonatore LM, Murphy BA, Wiltsie J, Chung CC, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, De Vita RJ, Pinto S, Nargund RP.
Bioorg Med Chem Lett (2019) 29 : 1380 -1385
PubMed 30952592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.77 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4585408 1 8.85
CHEMBL4452940 1 8.82
CHEMBL4531443 1 8.77
CHEMBL4453443 1 8.77
CHEMBL4557603 1 8.74
CHEMBL4458847 1 8.64
CHEMBL4543944 1 8.59
CHEMBL2408632 1 8.55
CHEMBL4483357 1 8.49
CHEMBL4467163 1 8.36
CHEMBL4572398 1 8.34
CHEMBL4460750 1 8.30
CHEMBL4443023 1 8.28
CHEMBL4592144 1 8.23
CHEMBL2408633 1 8.20
CHEMBL4530290 1 8.02
CHEMBL4453213 1 8.01
CHEMBL4464262 1 7.96
CHEMBL4461148 1 7.96
CHEMBL4561313 1 7.75
CHEMBL4534257 1 7.70
CHEMBL4476596 1 7.70
CHEMBL4554202 1 7.68
CHEMBL4461166 1 7.67
CHEMBL4473500 1 7.66
CHEMBL4467830 1 7.62
CHEMBL4527253 1 7.52
CHEMBL4562424 1 7.48
CHEMBL4516271 1 7.44
CHEMBL4527223 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4585408 IC50 = 1.4 nM 8.85
CHEMBL4452940 IC50 = 1.5 nM 8.82
CHEMBL4453443 IC50 = 1.7 nM 8.77
CHEMBL4531443 IC50 = 1.7 nM 8.77
CHEMBL4557603 IC50 = 1.8 nM 8.74
CHEMBL4458847 IC50 = 2.3 nM 8.64
CHEMBL4543944 IC50 = 2.6 nM 8.59
CHEMBL2408632 IC50 = 2.8 nM 8.55
CHEMBL4483357 IC50 = 3.2 nM 8.49
CHEMBL4467163 IC50 = 4.4 nM 8.36
CHEMBL4572398 IC50 = 4.6 nM 8.34
CHEMBL4460750 IC50 = 5.0 nM 8.30
CHEMBL4443023 IC50 = 5.2 nM 8.28
CHEMBL4592144 IC50 = 5.9 nM 8.23
CHEMBL2408633 IC50 = 6.3 nM 8.20
CHEMBL4530290 IC50 = 9.5 nM 8.02
CHEMBL4453213 IC50 = 9.8 nM 8.01
CHEMBL4464262 IC50 = 11.0 nM 7.96
CHEMBL4461148 IC50 = 11.0 nM 7.96
CHEMBL4561313 IC50 = 17.8 nM 7.75
CHEMBL4476596 IC50 = 20.0 nM 7.70
CHEMBL4534257 IC50 = 20.0 nM 7.70
CHEMBL4554202 IC50 = 21.0 nM 7.68
CHEMBL4461166 IC50 = 21.4 nM 7.67
CHEMBL4473500 IC50 = 22.0 nM 7.66
CHEMBL4467830 IC50 = 24.0 nM 7.62
CHEMBL4527253 IC50 = 30.0 nM 7.52
CHEMBL4562424 IC50 = 33.0 nM 7.48
CHEMBL4516271 IC50 = 36.0 nM 7.44
CHEMBL4527223 IC50 = 36.0 nM 7.44
CHEMBL4542552 IC50 = 38.1 nM 7.42
CHEMBL4469452 IC50 = 42.1 nM 7.38
CHEMBL4592655 IC50 = 46.0 nM 7.34
CHEMBL4461413 IC50 = 48.0 nM 7.32
CHEMBL4524803 IC50 = 78.0 nM 7.11
CHEMBL4577468 IC50 = 84.0 nM 7.08
CHEMBL4450287 IC50 = 108.0 nM 6.97
CHEMBL4531344 IC50 = 125.0 nM 6.90
CHEMBL4453600 IC50 = 247.0 nM 6.61
CHEMBL4462458 IC50 = 271.0 nM 6.57
CHEMBL4452750 IC50 = 528.0 nM 6.28
CHEMBL4565611 IC50 = 1908.0 nM 5.72