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Assay Detail

CHEMBL4309307

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

Functional
Antiproliferative activity against FRalpha knockout human IGROV1 KD10 cells after 96 hrs by Cell-Titer Blue assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

IGROV-1 (CHEMBL613984)
Type CELL-LINE
Organism Homo sapiens

Publication

Fluorine-Substituted Pyrrolo[2,3- d]Pyrimidine Analogues with Tumor Targeting via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis.
Ravindra M, Wilson MR, Tong N, O'Connor C, Karim M, Polin L, Wallace-Povirk A, White K, Kushner J, Hou Z, Matherly LH, Gangjee A.
J Med Chem (2018) 61 : 4228 -4248
PubMed 29701475 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.35 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4538151 1 7.72
CHEMBL225072 PEMETREXED 4.0 1 7.65
CHEMBL4214638 1 7.52
CHEMBL3628344 1 7.52
CHEMBL4445651 1 7.38
CHEMBL4465095 1 7.17
CHEMBL1834488 1 7.13
CHEMBL192632 1 6.72
CHEMBL365307 1 -
CHEMBL2158681 1 -
CHEMBL4540298 1 -
CHEMBL4557278 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4538151 IC50 = 19.2 nM 7.72
CHEMBL225072 PEMETREXED IC50 = 22.2 nM 7.65
CHEMBL4214638 IC50 = 30.5 nM 7.52
CHEMBL3628344 IC50 = 30.3 nM 7.52
CHEMBL4445651 IC50 = 42.2 nM 7.38
CHEMBL4465095 IC50 = 66.9 nM 7.17
CHEMBL1834488 IC50 = 74.6 nM 7.13
CHEMBL192632 IC50 = 190.0 nM 6.72
CHEMBL365307 IC50 > 1000.0 nM -
CHEMBL2158681 IC50 > 1000.0 nM -
CHEMBL4540298 IC50 > 1000.0 nM -
CHEMBL4557278 IC50 > 1000.0 nM -