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Compound Detail

CHEMBL5199976

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COc1cc(N=S2(=O)CCC2)cc2ncnc(Nc3cccnc3O[C@H]3COC[C@H]3O)c12

Basic Information

ChEMBL ID CHEMBL5199976
Phase Preclinical
Structure Type MOL
InChI Key GUXLMYYFWLSMCP-AEFFLSMTSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
2.42
ALogP
10
HBA
2
HBD
128.1
PSA (Ų)
0.57
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23N5O5S
MW 457.51
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.53

Activity Summary

IC50 4 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
IC50 7.96 6.46 11.0 2
MAP kinase-interacting serine/threonine-protein kinase 1
CHEMBL4718
IC50 6.98 6.98 104.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34533957 10.1021/acs.jmedchem.1c00368 MAP kinase-interacting serine/threonine-protein kinase 2 1
34533957 10.1021/acs.jmedchem.1c00368 MAP kinase-interacting serine/threonine-protein kinase 1 1

Data from ChEMBL 36 via Core Engine