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Compound Detail

CHEMBL1221640

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CCN(c1ccc2c(c1)C(C)(C)CCC2(C)C)c1ccc(-c2nnn[nH]2)cn1

Basic Information

ChEMBL ID CHEMBL1221640
Phase Preclinical
Structure Type MOL
InChI Key LAVVEKRPDLBLLX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

376.5
MW (Da)
4.77
ALogP
5
HBA
1
HBD
70.6
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 C22H28N6
MW 376.51
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.98

Activity Summary

EC50 1 meas. best 6.69

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor RXR-alpha
CHEMBL2061
EC50 6.69 6.69 205.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Retinoic acid receptor RXR-alpha EC50 = 205.0 nM 6.69 Agonist activity at RXRalpha by luciferase reporter gene assay 20656484

Literature References

PubMed DOI Target Context # Activities
20656484 10.1016/j.bmcl.2010.07.012 Retinoic acid receptor alpha 1
20656484 10.1016/j.bmcl.2010.07.012 Peroxisome proliferator-activated receptor gamma 1
20656484 10.1016/j.bmcl.2010.07.012 RXR alpha/PPAR gamma 1
20656484 10.1016/j.bmcl.2010.07.012 Oxysterols receptor LXR-alpha 1
20656484 10.1016/j.bmcl.2010.07.012 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha 1
20656484 10.1016/j.bmcl.2010.07.012 Retinoic acid receptor RXR-alpha 1

Data from ChEMBL 36 via Core Engine