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Compound Detail

CHEMBL350251

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N[C@@H]1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn4c3c2Oc2cc3c(ccc5ccccc53)cc2-4)C1

Basic Information

ChEMBL ID CHEMBL350251
Phase Preclinical
Structure Type MOL
InChI Key QYQUMHWYIJBNPE-MRXNPFEDSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

481.5
MW (Da)
4.78
ALogP
6
HBA
2
HBD
97.8
PSA (Ų)
0.35
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H20FN3O4
MW 481.48
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -0.14

Activity Summary

IC50 2 meas. best 5.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA polymerase I, thermostable
CHEMBL3564
IC50 5.62 5.62 2400.0 1
MCF7
CHEMBL387
IC50 5.37 5.37 4300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA polymerase I, thermostable IC50 = 2400.0 nM 5.62 Inhibition of Taq DNA polymerase 12570378
MCF7 IC50 = 4300.0 nM 5.37 Cytotoxicity of compound was tested against MCF-7 breast cancer cells 12570378

Literature References

PubMed DOI Target Context # Activities
12570378 10.1021/jm0203377 RPMI-8226 2
12570378 10.1021/jm0203377 NON-PROTEIN TARGET 1
12570378 10.1021/jm0203377 DNA topoisomerase II 1
12570378 10.1021/jm0203377 DNA polymerase I, thermostable 1
12570378 10.1021/jm0203377 MCF7 1

Data from ChEMBL 36 via Core Engine