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Compound Detail

CHEMBL105642

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COc1cc2c(Nc3ccc(Sc4nccn4C)c(Cl)c3)c(C#N)cnc2cc1OCCCN1CC[S+]([O-])CC1

Basic Information

ChEMBL ID CHEMBL105642
Phase Preclinical
Structure Type MOL
InChI Key SJIRAKJORBQMLF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

597.2
MW (Da)
5.23
ALogP
10
HBA
1
HBD
111.3
PSA (Ų)
0.19
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29ClN6O3S2
MW 597.17
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.58

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity mitogen-activated protein kinase kinase 1
CHEMBL3587
IC50 8.7 8.7 2.0 1
LoVo
CHEMBL614721
IC50 7.44 7.44 36.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12941327 10.1016/s0960-894x(03)00640-1 Dual specificity mitogen-activated protein kinase kinase 1 1
12941327 10.1016/s0960-894x(03)00640-1 LoVo 1
12941327 10.1016/s0960-894x(03)00640-1 Caco-2 1

Data from ChEMBL 36 via Core Engine