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Compound Detail

CHEMBL4072052

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Cc1cc(Nc2ccccc2)n2nc(SCc3nc4ccccc4[nH]3)nc2n1

Basic Information

ChEMBL ID CHEMBL4072052
Phase Preclinical
Structure Type MOL
InChI Key RPUPMJSUYBHUSL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

387.5
MW (Da)
4.34
ALogP
7
HBA
2
HBD
83.8
PSA (Ų)
0.44
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 C20H17N7S
MW 387.47
Aromatic Rings 5
Heavy Atoms 28
NP-Likeness -2.33

Activity Summary

IC50 1 meas. best 7.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ATP-dependent translocase ABCB1
CHEMBL4302
IC50 7.34 7.34 46.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30780087 10.1016/j.ejmech.2019.02.039 A549 7
30780087 10.1016/j.ejmech.2019.02.039 Lysine-specific histone demethylase 1A 6
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
30780087 10.1016/j.ejmech.2019.02.039 No relevant target 1
32683165 10.1016/j.ejmech.2020.112630 MGC-803 1
36724635 10.1016/j.ejmech.2023.115101 SW620/AD300 1

Data from ChEMBL 36 via Core Engine