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Assay Detail

CHEMBL5393235

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Functional
Antiproliferative activity against human KB cells assessed as cell growth inhibition incubated for 96 hrs by CellTiter-Blue cell viability assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KB
Confidence 1 — Organism
Curated By Autocuration

Target

KB (CHEMBL398)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of Tumor-Targeted 6-Methyl Substituted Pemetrexed and Related Antifolates with Selective Loss of RFC Transport.
Kaku K, Ravindra MP, Tong N, Choudhary S, Li X, Yu J, Karim M, Brzezinski M, O'Connor C, Hou Z, Matherly LH, Gangjee A.
ACS Med Chem Lett (2023) 14 : 1682 -1691
PubMed 38116433 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.28 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5398059 1 8.46
CHEMBL225072 PEMETREXED 4.0 1 8.00
CHEMBL5433810 1 7.54
CHEMBL374172 1 7.30
CHEMBL5417031 1 7.30
CHEMBL5416929 1 7.11
CHEMBL5404618 1 6.46
CHEMBL3407519 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5398059 IC50 = 3.43 nM 8.46
CHEMBL225072 PEMETREXED IC50 = 9.95 nM 8.00
CHEMBL5433810 IC50 = 28.5 nM 7.54
CHEMBL374172 IC50 = 49.49 nM 7.30
CHEMBL5417031 IC50 = 49.9 nM 7.30
CHEMBL5416929 IC50 = 77.31 nM 7.11
CHEMBL5404618 IC50 = 347.37 nM 6.46
CHEMBL3407519 IC50 = 833.0 nM 6.08