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Compound Detail

CHEMBL425350

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CN1CCN(CCC(=O)Nc2ccc3nc4ccc(NC(=O)CCN5CCN(C)CC5)cc4c(O)c3c2)CC1

Basic Information

ChEMBL ID CHEMBL425350
Phase Preclinical
Structure Type MOL
InChI Key SGXMRPFOHAFYSL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

533.7
MW (Da)
2.25
ALogP
8
HBA
3
HBD
104.3
PSA (Ų)
0.38
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H39N7O3
MW 533.68
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.89

Activity Summary

EC50 1 meas. best 5.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Telomerase reverse transcriptase
CHEMBL2916
EC50 5.72 5.72 1900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Telomerase reverse transcriptase EC50 = 1900.0 nM 5.72 Concentration required to inhibit 50% of telomerase activity 15501053

Literature References

PubMed DOI Target Context # Activities
15501053 10.1016/j.bmcl.2004.09.037 Telomerase reverse transcriptase 1
15501053 10.1016/j.bmcl.2004.09.037 A2780 1
15501053 10.1016/j.bmcl.2004.09.037 NON-PROTEIN TARGET 1
15501053 10.1016/j.bmcl.2004.09.037 SK-OV-3 1

Data from ChEMBL 36 via Core Engine