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Compound Detail

CHEMBL4530032

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CCCN1CCC(c2nc3c(C(N)=O)c(F)ccc3[nH]2)CC1

Basic Information

ChEMBL ID CHEMBL4530032
Phase Preclinical
Structure Type MOL
InChI Key CRTMDBOMSUUNQZ-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

304.4
MW (Da)
2.39
ALogP
3
HBA
2
HBD
75.0
PSA (Ų)
0.91
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H21FN4O
MW 304.37
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -1.67

Activity Summary

IC50 3 meas. best 7.53

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Poly [ADP-ribose] polymerase 1
CHEMBL3105
IC50 7.53 7.53 29.8 1
HCT-116
CHEMBL394
IC50 4.18 4.18 65500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Poly [ADP-ribose] polymerase 1 IC50 = 29.8 nM 7.53 Inhibition of PARP1 (unknown origin) 27353531
HCT-116 IC50 = 65500.0 nM 4.18 Cytotoxicity against human HCT116 cells by SRB assay 27353531

Literature References

PubMed DOI Target Context # Activities
27353531 10.1016/j.bmcl.2016.06.045 Poly [ADP-ribose] polymerase 1 4
27353531 10.1016/j.bmcl.2016.06.045 HCT-116 1

Data from ChEMBL 36 via Core Engine