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Compound Detail

CHEMBL288229

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CCSCc1ccc2c(c1)c1c3c(c4c5ccccc5n5c4c1n2[C@@]1(C)O[C@@H]5C[C@]1(O)C(=O)OC)C(=O)NC3

Basic Information

ChEMBL ID CHEMBL288229
Phase Preclinical
Structure Type MOL
InChI Key UFLRHQRKTYVKGB-RIGQTMPJSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

541.6
MW (Da)
4.91
ALogP
8
HBA
2
HBD
94.7
PSA (Ų)
0.31
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H27N3O5S
MW 541.63
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness 0.59

Activity Summary

IC50 5 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 11
CHEMBL2708
IC50 7.68 7.68 21.0 1
Mitogen-activated protein kinase kinase kinase 9
CHEMBL2872
IC50 7.55 7.55 28.0 1
Mitogen-activated protein kinase kinase kinase 10
CHEMBL2873
IC50 7.55 7.55 28.0 1
High affinity nerve growth factor receptor
CHEMBL2815
IC50 7.21 7.21 61.0 1
Protein kinase C (PKC)
CHEMBL2094266
IC50 6.4 6.4 400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11755341 10.1016/s0960-894x(01)00690-4 Mitogen-activated protein kinase kinase kinase 9 1
11755341 10.1016/s0960-894x(01)00690-4 Mitogen-activated protein kinase kinase kinase 10 1
11755341 10.1016/s0960-894x(01)00690-4 Mitogen-activated protein kinase kinase kinase 11 1
11755341 10.1016/s0960-894x(01)00690-4 Protein kinase C (PKC) 1
11755341 10.1016/s0960-894x(01)00690-4 High affinity nerve growth factor receptor 1

Data from ChEMBL 36 via Core Engine