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Compound Detail

CHEMBL93823

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COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)c2[nH]c(C3CC3)nc12

Basic Information

ChEMBL ID CHEMBL93823
Phase Preclinical
Structure Type MOL
InChI Key SLPPCYGGTCSDJX-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

377.2
MW (Da)
4.40
ALogP
4
HBA
2
HBD
79.9
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14Cl2N4O2
MW 377.23
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.04

Activity Summary

IC50 1 meas. best 8.7
Ki 1 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 9.0 9.0 1.0 1
Phosphodiesterase 4
CHEMBL2093863
IC50 8.7 8.7 2.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 1.0 nM 9.0 Inhibition of Rolipram binding to PDE4 9873613
Phosphodiesterase 4 IC50 = 2.0 nM 8.7 Inhibition of PDE4 from guinea pig macrophages 9873613

Literature References

PubMed DOI Target Context # Activities
9873613 10.1016/s0960-894x(98)00497-1 Phosphodiesterase 4 1
9873613 10.1016/s0960-894x(98)00497-1 Unchecked 1

Data from ChEMBL 36 via Core Engine