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Compound Detail

CHEMBL3814550

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C[C@@H]1CC(=O)Nc2cccc(-c3ccc4c(c3)c(C3CC3)nn4C)c2N1

Basic Information

ChEMBL ID CHEMBL3814550
Phase Preclinical
Structure Type MOL
InChI Key RUOHSEWJRWMCPQ-GFCCVEGCSA-N
2
Targets
5
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

346.4
MW (Da)
4.26
ALogP
4
HBA
2
HBD
59.0
PSA (Ų)
0.73
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22N4O
MW 346.43
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.36

Activity Summary

IC50 4 meas. best 7.48
EC50 1 meas. best 5.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CREB-binding protein
CHEMBL5747
IC50 7.48 7.395 33.0 2
CREB-binding protein
CHEMBL5747
EC50 5.52 5.52 3000.0 1
Bromodomain-containing protein 4
CHEMBL1163125
IC50 5.39 5.22 4028.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27190605 10.1021/acsmedchemlett.6b00075 CREB-binding protein 3
27190605 10.1021/acsmedchemlett.6b00075 Bromodomain-containing protein 4 1

Data from ChEMBL 36 via Core Engine