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Compound Detail

CHEMBL202801

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CCc1cc(Nc2cc(=O)n(CCCCN3CCN(c4cc5c(cc4F)c(=O)c(C(=O)O)cn5-c4ccc(F)cc4)CC3)c(=O)[nH]2)ccc1C

Basic Information

ChEMBL ID CHEMBL202801
Phase Preclinical
Structure Type MOL
InChI Key PXGPMQZETUARJW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

684.7
MW (Da)
5.03
ALogP
9
HBA
3
HBD
132.7
PSA (Ų)
0.17
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H38F2N6O5
MW 684.74
Aromatic Rings 5
Heavy Atoms 50
NP-Likeness -1.18

Activity Summary

Ki 1 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA polymerase III PolC-type
CHEMBL3897
Ki 7.77 7.77 17.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA polymerase III PolC-type Ki = 17.0 nM 7.77 Binding affinity to Bacillus subtilis DNA polymerase3C 16480282

Literature References

PubMed DOI Target Context # Activities
16480282 10.1021/jm0510023 Staphylococcus aureus 3
16480282 10.1021/jm0510023 Enterococcus faecium 2
16480282 10.1021/jm0510023 DNA polymerase III PolC-type 1
16480282 10.1021/jm0510023 Bacillus subtilis 1
16480282 10.1021/jm0510023 Enterococcus faecalis 1
16480282 10.1021/jm0510023 Escherichia coli 1

Data from ChEMBL 36 via Core Engine