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Assay Detail

CHEMBL2183606

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human recombinant DGAT1 expressed in Sf9 cells by liquid scintillography
ChEMBL ↗
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Diacylglycerol O-acyltransferase 1 (CHEMBL6009) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
Barlind JG, Bauer UA, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RD, Eriksson JW, Hammond CD, Hovland R, Johannesson P, Johansson MJ, Kemmitt PD, Lindmark BT, Morentin Gutierrez P, Noeske TA, Nordin A, O'Donnell CJ, Petersson AU, Redzic A, Turnbull AV, Vinblad J.
J Med Chem (2012) 55 : 10610 -10629
PubMed 23116186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 6.47 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178943 — — 1 7.52
CHEMBL2178947 — — 1 7.52
CHEMBL2178369 — — 1 7.52
CHEMBL2178373 — — 1 7.40
CHEMBL2178940 — — 1 7.22
CHEMBL2178942 — — 1 7.22
CHEMBL2178946 — — 1 7.16
CHEMBL4297354 AZD-7687 1.0 1 7.10
CHEMBL2178371 — — 1 7.10
CHEMBL2178939 — — 1 7.00
CHEMBL2178937 — — 1 6.96
CHEMBL2178384 — — 1 6.96
CHEMBL2178945 — — 1 6.92
CHEMBL2178370 — — 1 6.92
CHEMBL2178941 — — 1 6.92
CHEMBL2178948 — — 1 6.77
CHEMBL2178372 — — 1 6.70
CHEMBL2178949 — — 1 6.62
CHEMBL2178951 — — 1 6.51
CHEMBL2178388 — — 1 6.39
CHEMBL2178944 — — 1 6.37
CHEMBL2178935 — — 1 6.28
CHEMBL2178954 — — 1 6.23
CHEMBL2178933 — — 1 6.16
CHEMBL2178950 — — 1 5.96
CHEMBL2178938 — — 1 5.96
CHEMBL2178934 — — 1 5.92
CHEMBL2178389 — — 1 5.75
CHEMBL2178936 — — 1 5.72
CHEMBL2178952 — — 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178943 — IC50 = 30.0 nM 7.52
CHEMBL2178369 — IC50 = 30.0 nM 7.52
CHEMBL2178947 — IC50 = 30.0 nM 7.52
CHEMBL2178373 — IC50 = 40.0 nM 7.40
CHEMBL2178940 — IC50 = 60.0 nM 7.22
CHEMBL2178942 — IC50 = 60.0 nM 7.22
CHEMBL2178946 — IC50 = 70.0 nM 7.16
CHEMBL4297354 AZD-7687 IC50 = 80.0 nM 7.10
CHEMBL2178371 — IC50 = 80.0 nM 7.10
CHEMBL2178939 — IC50 = 100.0 nM 7.00
CHEMBL2178937 — IC50 = 110.0 nM 6.96
CHEMBL2178384 — IC50 = 110.0 nM 6.96
CHEMBL2178370 — IC50 = 120.0 nM 6.92
CHEMBL2178941 — IC50 = 120.0 nM 6.92
CHEMBL2178945 — IC50 = 120.0 nM 6.92
CHEMBL2178948 — IC50 = 170.0 nM 6.77
CHEMBL2178372 — IC50 = 200.0 nM 6.70
CHEMBL2178949 — IC50 = 240.0 nM 6.62
CHEMBL2178951 — IC50 = 310.0 nM 6.51
CHEMBL2178388 — IC50 = 410.0 nM 6.39
CHEMBL2178944 — IC50 = 430.0 nM 6.37
CHEMBL2178935 — IC50 = 520.0 nM 6.28
CHEMBL2178954 — IC50 = 590.0 nM 6.23
CHEMBL2178933 — IC50 = 690.0 nM 6.16
CHEMBL2178950 — IC50 = 1100.0 nM 5.96
CHEMBL2178938 — IC50 = 1100.0 nM 5.96
CHEMBL2178934 — IC50 = 1200.0 nM 5.92
CHEMBL2178389 — IC50 = 1800.0 nM 5.75
CHEMBL2178936 — IC50 = 1900.0 nM 5.72
CHEMBL2178952 — IC50 = 1900.0 nM 5.72
CHEMBL2178386 — IC50 = 28000.0 nM 4.55
CHEMBL2178387 — IC50 = 41000.0 nM 4.39
CHEMBL2178385 — IC50 = 60000.0 nM 4.22
CHEMBL2178391 — IC50 > 10000.0 nM -
CHEMBL2178390 — IC50 > 10000.0 nM -
CHEMBL2178930 — IC50 > 9100.0 nM -
CHEMBL2178931 — IC50 > 10000.0 nM -
CHEMBL2178383 — IC50 - — -
CHEMBL2178382 — IC50 > 33000.0 nM -
CHEMBL2178392 — IC50 > 10000.0 nM -
CHEMBL2178380 — IC50 - — -
CHEMBL2178379 — IC50 - — -
CHEMBL2178378 — IC50 - — -
CHEMBL2178377 — IC50 - — -
CHEMBL2178376 — IC50 - — -
CHEMBL2178375 — IC50 - — -
CHEMBL2178932 — IC50 > 10000.0 nM -
CHEMBL2178381 — IC50 - — -