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Compound Detail

CHEMBL5180553

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O=c1nc2n(c3c1CN(Cc1ccccc1)CC3)CCN2Cc1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL5180553
Phase Preclinical
Structure Type MOL
InChI Key DFGQUMJGXYWZSB-UHFFFAOYSA-N
7
Targets
7
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

390.5
MW (Da)
2.96
ALogP
5
HBA
0
HBD
41.4
PSA (Ų)
0.69
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H23FN4O
MW 390.46
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.38

Activity Summary

IC50 6 meas. best 7.1
EC50 1 meas. best 6.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HCT-116
CHEMBL394
IC50 7.1 7.1 80.0 1
DLD-1
CHEMBL614285
IC50 7.05 7.05 90.0 1
ATP-dependent Clp protease proteolytic subunit, mitochondrial
CHEMBL4523305
EC50 6.89 6.89 130.0 1
SW480
CHEMBL612544
IC50 6.77 6.77 170.0 1
SW-620
CHEMBL612262
IC50 6.72 6.72 190.0 1
HCT-15
CHEMBL612263
IC50 6.68 6.68 210.0 1
HT-29
CHEMBL384
IC50 6.4 6.4 400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35609303 10.1021/acs.jmedchem.1c02071 ATP-dependent Clp protease proteolytic subunit, mitochondrial 2
35609303 10.1021/acs.jmedchem.1c02071 HCT-116 1
35609303 10.1021/acs.jmedchem.1c02071 HT-29 1
35609303 10.1021/acs.jmedchem.1c02071 SW-620 1
35609303 10.1021/acs.jmedchem.1c02071 DLD-1 1
35609303 10.1021/acs.jmedchem.1c02071 HCT-15 1
35609303 10.1021/acs.jmedchem.1c02071 SW480 1

Data from ChEMBL 36 via Core Engine