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Compound Detail

CHEMBL99494

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Cc1ccccc1-n1c(=O)n(Cc2cccs2)c(=O)c2[nH]cnc21

Basic Information

ChEMBL ID CHEMBL99494
Phase Preclinical
Structure Type MOL
InChI Key LAKMUAOMXHIOEY-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

338.4
MW (Da)
2.29
ALogP
6
HBA
1
HBD
72.7
PSA (Ų)
0.62
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14N4O2S
MW 338.39
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.85

Activity Summary

IC50 3 meas. best 5.99
Ki 1 meas. best 5.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 5.99 5.685 1020.0 2
Unchecked
CHEMBL612545
Ki 5.99 5.99 1020.0 1
Unchecked
CHEMBL612545
IC50 5.38 5.38 4200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphodiesterase 4 IC50 = 1020.0 nM 5.99 Inhibition of rolipram binding 9873649
Unchecked Ki = 1020.0 nM 5.99 Displacement of [3H]rolipram from PDE4 by RBA 18686943
Phosphodiesterase 4 IC50 = 4200.0 nM 5.38 Inhibition of PDE4 9873649
Unchecked IC50 = 4200.0 nM 5.38 Inhibition of PDE4 18686943

Literature References

PubMed DOI Target Context # Activities
9873649 10.1016/s0960-894x(98)00524-1 Phosphodiesterase 4 3
9873649 10.1016/s0960-894x(98)00524-1 Cavia porcellus 2
18686943 10.1021/jm800582j Unchecked 2
9873649 10.1016/s0960-894x(98)00524-1 Mustela putorius furo 1

Data from ChEMBL 36 via Core Engine