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Assay Detail

CHEMBL640282

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

Binding
Inhibitory activity against rat ATP-citrate lyase activity by the maleate dehydrogenase catalyzed reduction of oxaloacetate by NADH.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

ATP-citrate synthase (CHEMBL2745)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

ATP-citrate lyase as a target for hypolipidemic intervention. Design and synthesis of 2-substituted butanedioic acids as novel, potent inhibitors of the enzyme.
Gribble AD, Dolle RE, Shaw A, McNair D, Novelli R, Novelli CE, Slingsby BP, Shah VP, Tew D, Saxty BA, Allen M, Groot PH, Pearce N, Yates J.
J Med Chem (1996) 39 : 3569 -3584
PubMed 8784456 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 4.77 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121948 1 5.92
CHEMBL118918 1 5.58
CHEMBL333756 1 5.54
CHEMBL116883 1 5.54
CHEMBL119690 1 5.14
CHEMBL120840 1 5.14
CHEMBL118149 1 5.13
CHEMBL120379 1 5.00
CHEMBL118890 1 4.98
CHEMBL118737 1 4.92
CHEMBL120848 1 4.75
CHEMBL118961 1 4.68
CHEMBL120795 1 4.60
CHEMBL422789 1 4.60
CHEMBL120604 1 4.51
CHEMBL120510 1 4.48
CHEMBL333104 1 4.42
CHEMBL118670 1 4.19
CHEMBL331542 1 4.17
CHEMBL120202 1 4.16
CHEMBL119988 1 4.15
CHEMBL332398 1 4.12
CHEMBL118920 1 4.06
CHEMBL118632 1 -
CHEMBL116658 1 -
CHEMBL325929 1 -
CHEMBL333172 1 -
CHEMBL120624 1 -
CHEMBL120378 1 -
CHEMBL116544 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121948 Ki = 1200.0 nM 5.92
CHEMBL118918 Ki = 2600.0 nM 5.58
CHEMBL116883 Ki = 2900.0 nM 5.54
CHEMBL333756 Ki = 2900.0 nM 5.54
CHEMBL119690 Ki = 7300.0 nM 5.14
CHEMBL120840 Ki = 7200.0 nM 5.14
CHEMBL118149 Ki = 7400.0 nM 5.13
CHEMBL120379 Ki = 10000.0 nM 5.00
CHEMBL118890 Ki = 10500.0 nM 4.98
CHEMBL118737 Ki = 12000.0 nM 4.92
CHEMBL120848 Ki = 18000.0 nM 4.75
CHEMBL118961 Ki = 21000.0 nM 4.68
CHEMBL120795 Ki = 25000.0 nM 4.60
CHEMBL422789 Ki = 25000.0 nM 4.60
CHEMBL120604 Ki = 31000.0 nM 4.51
CHEMBL120510 Ki = 33000.0 nM 4.48
CHEMBL333104 Ki = 38000.0 nM 4.42
CHEMBL118670 Ki = 64000.0 nM 4.19
CHEMBL331542 Ki = 67000.0 nM 4.17
CHEMBL120202 Ki = 69000.0 nM 4.16
CHEMBL119988 Ki = 71000.0 nM 4.15
CHEMBL332398 Ki = 76000.0 nM 4.12
CHEMBL118920 Ki = 88000.0 nM 4.06
CHEMBL418864 Ki = 130000.0 nM -
CHEMBL331020 Ki = 420000.0 nM -
CHEMBL331482 Ki = 120000.0 nM -
CHEMBL118935 Ki = 175000.0 nM -
CHEMBL120603 Ki = 500000.0 nM -
CHEMBL121149 Ki = 410000.0 nM -
CHEMBL331622 Ki = 178000.0 nM -
CHEMBL116544 Ki = 150000.0 nM -
CHEMBL120378 Ki = 131000.0 nM -
CHEMBL120624 Ki = 420000.0 nM -
CHEMBL333172 Ki = 300000.0 nM -
CHEMBL325929 Ki = 490000.0 nM -
CHEMBL116658 Ki = 226000.0 nM -
CHEMBL118632 Ki = 110000.0 nM -