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Compound Detail

CHEMBL2177791

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COc1cc2c(cc1O)C(=O)c1c-2n(CCCN2CCOCC2)c(=O)c2cc(OC)c(OC)cc12

Basic Information

ChEMBL ID CHEMBL2177791
Phase Preclinical
Structure Type MOL
InChI Key DIZYBTAYMOFSCR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

480.5
MW (Da)
2.67
ALogP
9
HBA
1
HBD
99.5
PSA (Ų)
0.43
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H28N2O7
MW 480.52
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness 0.05

Activity Summary

IC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CWR22R
CHEMBL612657
IC50 8.7 8.7 2.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CWR22R IC50 = 2.0 nM 8.7 Cytotoxicity against human 22Rv1 cells after 2 hrs by [3H]thymidine incorporatio... 25822623

Literature References

PubMed DOI Target Context # Activities
25822623 10.1021/jm5018384 Mus musculus 3
25822623 10.1021/jm5018384 CWR22R 2
23215354 10.1021/jm300519w DNA topoisomerase 1 1
23215354 10.1021/jm300519w MCF7 1
23215354 10.1021/jm300519w DU-145 1
23215354 10.1021/jm300519w SN12C 1
23215354 10.1021/jm300519w OVCAR-3 1
23215354 10.1021/jm300519w UACC-62 1
23215354 10.1021/jm300519w SF-539 1
23215354 10.1021/jm300519w HCT-116 1
23215354 10.1021/jm300519w HOP-62 1
25811317 10.1021/acs.jmedchem.5b00136 Tyrosyl-DNA phosphodiesterase 1 1

Data from ChEMBL 36 via Core Engine