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Compound Detail

CHEMBL1221641

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CCN(c1ccc2c(c1)C(C)(C)CCC2(C)C)c1ccc(C(=O)O)cn1

Basic Information

ChEMBL ID CHEMBL1221641
Phase Preclinical
Structure Type MOL
InChI Key RXCTZCYFGJAJCU-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

352.5
MW (Da)
5.29
ALogP
3
HBA
1
HBD
53.4
PSA (Ų)
0.81
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28N2O2
MW 352.48
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.32

Activity Summary

EC50 4 meas. best 8.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor RXR-alpha
CHEMBL2061
EC50 8.42 8.3267 3.8 3
Retinoid X receptor
CHEMBL2363070
EC50 7.86 7.86 13.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24900488 10.1021/ml300055n Mus musculus 18
27592633 10.1021/acs.jmedchem.6b00812 Retinoid X receptor 5
23391145 10.1021/jm400033f Retinoic acid receptor RXR-alpha 5
24900241 10.1021/ml100184k Retinoic acid receptor RXR-alpha 4
27592633 10.1021/acs.jmedchem.6b00812 Retinoic acid receptor RXR-alpha 3
23391145 10.1021/jm400033f Mus musculus 3
36923911 10.1021/acsmedchemlett.2c00509 Retinoic acid receptor RXR-alpha 3
27592633 10.1021/acs.jmedchem.6b00812 Unchecked 2
27592633 10.1021/acs.jmedchem.6b00812 HuT78 2
27592633 10.1021/acs.jmedchem.6b00812 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha 2
24900488 10.1021/ml300055n Peroxisome proliferator-activated receptor gamma 1
24900488 10.1021/ml300055n Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha 1
24900488 10.1021/ml300055n Oxysterols receptor LXR-alpha 1
24900488 10.1021/ml300055n RXR alpha/PPAR gamma 1
20656484 10.1016/j.bmcl.2010.07.012 Retinoic acid receptor alpha 1
24900241 10.1021/ml100184k Oxysterols receptor LXR-alpha 1
24900241 10.1021/ml100184k Peroxisome proliferator-activated receptor gamma 1
20656484 10.1016/j.bmcl.2010.07.012 Oxysterols receptor LXR-alpha 1
20656484 10.1016/j.bmcl.2010.07.012 RXR alpha/PPAR gamma 1
20656484 10.1016/j.bmcl.2010.07.012 Peroxisome proliferator-activated receptor gamma 1

Data from ChEMBL 36 via Core Engine