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Assay Detail

CHEMBL906357

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Binding
Inhibition of human recombinant ATP-citrate lyase
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

ATP-citrate synthase (CHEMBL3720)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.
Li JJ, Wang H, Tino JA, Robl JA, Herpin TF, Lawrence RM, Biller S, Jamil H, Ponticiello R, Chen L, Chu CH, Flynn N, Cheng D, Zhao R, Chen B, Schnur D, Obermeier MT, Sasseville V, Padmanabha R, Pike K, Harrity T.
Bioorg Med Chem Lett (2007) 17 : 3208 -3211
PubMed 17383874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.86 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399379 1 6.89
CHEMBL118715 1 6.82
CHEMBL400743 1 6.72
CHEMBL250942 1 6.47
CHEMBL250941 1 6.43
CHEMBL249069 1 5.96
CHEMBL119628 1 5.68
CHEMBL398749 1 5.64
CHEMBL400562 1 5.25
CHEMBL399634 1 5.16
CHEMBL249272 1 5.12
CHEMBL250745 1 5.09
CHEMBL250744 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399379 IC50 = 130.0 nM 6.89
CHEMBL118715 IC50 = 150.0 nM 6.82
CHEMBL400743 IC50 = 190.0 nM 6.72
CHEMBL250942 IC50 = 340.0 nM 6.47
CHEMBL250941 IC50 = 370.0 nM 6.43
CHEMBL249069 IC50 = 1100.0 nM 5.96
CHEMBL119628 IC50 = 2100.0 nM 5.68
CHEMBL398749 IC50 = 2300.0 nM 5.64
CHEMBL400562 IC50 = 5600.0 nM 5.25
CHEMBL399634 IC50 = 6900.0 nM 5.16
CHEMBL249272 IC50 = 7600.0 nM 5.12
CHEMBL250745 IC50 = 8100.0 nM 5.09
CHEMBL250744 IC50 = 10900.0 nM 4.96