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Assay Detail

CHEMBL685744

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

Functional
Activity was evaluated against HCT-8 tumor cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-8
Confidence 1 — Organism
Curated By Expert

Target

HCT-8 (CHEMBL613510)
Type CELL-LINE
Organism Homo sapiens

Publication

High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
Kuyper LF, Baccanari DP, Jones ML, Hunter RN, Tansik RL, Joyner SS, Boytos CM, Rudolph SK, Knick V, Wilson HR, Caddell JM, Friedman HS, Comley JC, Stables JN.
J Med Chem (1996) 39 : 892 -903
PubMed 8632413 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.43 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL352960 1 9.24
CHEMBL170144 1 9.23
CHEMBL170758 1 9.13
CHEMBL171765 1 9.12
CHEMBL170760 1 9.09
CHEMBL170837 1 8.89
CHEMBL369258 1 8.89
CHEMBL170654 1 8.85
CHEMBL119 TRIMETREXATE 4.0 1 8.74
CHEMBL424170 1 8.68
CHEMBL353763 1 8.51
CHEMBL171305 1 8.48
CHEMBL171494 1 8.36
CHEMBL318721 1 8.22
CHEMBL173617 1 8.13
CHEMBL170900 1 8.10
CHEMBL171629 1 7.28
CHEMBL353929 1 7.07
CHEMBL174414 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL352960 IC50 = 0.57 nM 9.24
CHEMBL170144 IC50 = 0.59 nM 9.23
CHEMBL170758 IC50 = 0.74 nM 9.13
CHEMBL171765 IC50 = 0.75 nM 9.12
CHEMBL170760 IC50 = 0.82 nM 9.09
CHEMBL170837 IC50 = 1.3 nM 8.89
CHEMBL369258 IC50 = 1.3 nM 8.89
CHEMBL170654 IC50 = 1.4 nM 8.85
CHEMBL119 TRIMETREXATE IC50 = 1.8 nM 8.74
CHEMBL424170 IC50 = 2.1 nM 8.68
CHEMBL353763 IC50 = 3.1 nM 8.51
CHEMBL171305 IC50 = 3.3 nM 8.48
CHEMBL171494 IC50 = 4.4 nM 8.36
CHEMBL318721 IC50 = 6.0 nM 8.22
CHEMBL173617 IC50 = 7.4 nM 8.13
CHEMBL170900 IC50 = 8.0 nM 8.10
CHEMBL171629 IC50 = 52.0 nM 7.28
CHEMBL353929 IC50 = 85.0 nM 7.07
CHEMBL174414 IC50 = 580.0 nM 6.24