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Assay Detail

CHEMBL4224229

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Functional
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HL-60
Confidence 1 — Organism
Curated By Intermediate

Target

HL-60 (CHEMBL383)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase.
Madak JT, Cuthbertson CR, Miyata Y, Tamura S, Petrunak EM, Stuckey JA, Han Y, He M, Sun D, Showalter HD, Neamati N.
J Med Chem (2018) 61 : 5162 -5186
PubMed 29727569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.41 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4227747 1 6.40
CHEMBL38434 BREQUINAR 2.0 1 6.26
CHEMBL4227217 1 5.57
CHEMBL3600460 1 5.46
CHEMBL4228971 1 5.32
CHEMBL4224965 1 5.15
CHEMBL4227722 1 5.15
CHEMBL4228712 1 5.03
CHEMBL4226472 1 4.94
CHEMBL4225759 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4227747 IC50 = 401.0 nM 6.40
CHEMBL38434 BREQUINAR IC50 = 544.0 nM 6.26
CHEMBL4227217 IC50 = 2670.0 nM 5.57
CHEMBL3600460 IC50 = 3510.0 nM 5.46
CHEMBL4228971 IC50 = 4810.0 nM 5.32
CHEMBL4224965 IC50 = 7120.0 nM 5.15
CHEMBL4227722 IC50 = 7080.0 nM 5.15
CHEMBL4228712 IC50 = 9280.0 nM 5.03
CHEMBL4226472 IC50 = 11600.0 nM 4.94
CHEMBL4225759 IC50 = 15300.0 nM 4.82