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Compound Detail

CHEMBL4207978

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CC(C)(C)c1cc(-c2cc(-c3ccc(C(=O)O)cc3)ccc2OCCO)ccc1NCCCCO

Basic Information

ChEMBL ID CHEMBL4207978
Phase Preclinical
Structure Type MOL
InChI Key XMIDMHMHZMEFOR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

477.6
MW (Da)
5.57
ALogP
5
HBA
4
HBD
99.0
PSA (Ų)
0.27
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H35NO5
MW 477.60
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.21

Activity Summary

EC50 1 meas. best 7.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor gamma
CHEMBL2003
EC50 7.17 7.17 67.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.0001 - Not specified

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29706423 10.1016/j.bmcl.2018.04.036 Unchecked 2
29706423 10.1016/j.bmcl.2018.04.036 Retinoic acid receptor gamma 1
29706423 10.1016/j.bmcl.2018.04.036 Retinoic acid receptor alpha 1
29706423 10.1016/j.bmcl.2018.04.036 Retinoic acid receptor beta 1
29706423 10.1016/j.bmcl.2018.04.036 Hepatocyte 1
29706423 10.1016/j.bmcl.2018.04.036 ADMET 1

Data from ChEMBL 36 via Core Engine