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Compound Detail

CHEMBL99039

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CC1(C)N=C(N)N=C(N)N1c1ccc(CCCCc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL99039
Phase Preclinical
Structure Type MOL
InChI Key RHDNKXYQUZIPEI-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

349.5
MW (Da)
3.44
ALogP
5
HBA
2
HBD
80.0
PSA (Ų)
0.78
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H27N5
MW 349.48
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.17

Activity Summary

IC50 3 meas. best 4.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine protein phosphatase PP2B-alpha catalytic subunit
CHEMBL5278
IC50 4.3 4.3 50000.0 1
Unchecked
CHEMBL612545
IC50 4.3 4.3 50000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 50000.0 nM 4.3 Inhibition of PP2A 16509582
Serine/threonine protein phosphatase PP2B-alpha catalytic subunit IC50 = 50000.0 nM 4.3 Inhibition of PP2B 16509582
Unchecked IC50 = 50000.0 nM 4.3 Inhibition of PP1 16509582

Literature References

PubMed DOI Target Context # Activities
16509582 10.1021/jm051033y Unchecked 2
1895302 10.1021/jm00113a022 Dihydrofolate reductase 1
16509582 10.1021/jm051033y Serine/threonine protein phosphatase PP2B-alpha catalytic subunit 1

Data from ChEMBL 36 via Core Engine