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Compound Detail

CHEMBL4060656

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Cc1ccc(Nc2cc(C)nc3nc(SCc4nc5ccccc5[nH]4)nn23)cc1

Basic Information

ChEMBL ID CHEMBL4060656
Phase Preclinical
Structure Type MOL
InChI Key UKHSKMVFGGAFFY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

401.5
MW (Da)
4.65
ALogP
7
HBA
2
HBD
83.8
PSA (Ų)
0.42
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H19N7S
MW 401.50
Aromatic Rings 5
Heavy Atoms 29
NP-Likeness -2.37

Activity Summary

IC50 1 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ATP-dependent translocase ABCB1
CHEMBL4302
IC50 6.3 6.3 500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33280384 10.1021/acs.jmedchem.0c01741 ATP-dependent translocase ABCB1 2
27769034 10.1016/j.ejmech.2016.10.021 MGC-803 1
27769034 10.1016/j.ejmech.2016.10.021 ECa-109 cell line 1
27769034 10.1016/j.ejmech.2016.10.021 A549 1
27769034 10.1016/j.ejmech.2016.10.021 PC-9 1
27769034 10.1016/j.ejmech.2016.10.021 Lysine-specific histone demethylase 1A 1

Data from ChEMBL 36 via Core Engine