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Compound Detail

CHEMBL2059872

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Cc1ccc(-c2ncc(CN3CCOCC3)s2)cc1NC(=O)c1ccc(OCc2ccccn2)cc1

Basic Information

ChEMBL ID CHEMBL2059872
Phase Preclinical
Structure Type MOL
InChI Key FPCRNQDPAAFAKL-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

500.6
MW (Da)
5.18
ALogP
7
HBA
1
HBD
76.6
PSA (Ų)
0.36
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H28N4O3S
MW 500.62
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -2.19

Activity Summary

IC50 2 meas. best 7.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein smoothened
CHEMBL5971
IC50 7.38 7.38 42.0 1
Mitogen-activated protein kinase 14
CHEMBL260
IC50 4.52 4.52 30000.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.033 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22704236 10.1016/j.bmcl.2012.04.104 Protein smoothened 2
22704236 10.1016/j.bmcl.2012.04.104 Mitogen-activated protein kinase 14 1
22704236 10.1016/j.bmcl.2012.04.104 No relevant target 1
22704236 10.1016/j.bmcl.2012.04.104 Plasma 1
- 10.6019/CHEMBL3301361 No relevant target 1
- 10.6019/CHEMBL3301361 ADMET 1

Data from ChEMBL 36 via Core Engine