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Compound Detail

CHEMBL311269

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CC(C)N1CCC(C)(C)c2cc(C#Cc3ccc(C(=O)O)cc3)ccc21

Basic Information

ChEMBL ID CHEMBL311269
Phase Preclinical
Structure Type MOL
InChI Key OCMSZODRCJAGHL-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

347.5
MW (Da)
4.68
ALogP
2
HBA
1
HBD
40.5
PSA (Ų)
0.80
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 C23H25NO2
MW 347.46
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.14

Activity Summary

Kd 3 meas. best 7.22
EC50 2 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor gamma
CHEMBL2003
EC50 8.22 8.22 6.0 1
Retinoic acid receptor beta
CHEMBL2008
EC50 8.0 8.0 10.0 1
Retinoic acid receptor beta
CHEMBL2008
Kd 7.22 7.22 60.0 1
Retinoic acid receptor gamma
CHEMBL2003
Kd 7.14 7.14 72.0 1
Retinoic acid receptor alpha
CHEMBL2055
Kd 6.2 6.2 627.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4689842 HEK-293T 346
- 10.6019/CHEMBL4689842 U2OS 345
- 10.6019/CHEMBL4689842 Fibroblast 344
- 10.1016/S0960-894X(97)00435-6 Retinoic acid receptor alpha 2
- 10.1016/S0960-894X(97)00435-6 Retinoic acid receptor beta 2
- 10.1016/S0960-894X(97)00435-6 Retinoic acid receptor gamma 2
- 10.6019/CHEMBL5060014 Tyrosine-protein kinase ABL1 1
- 10.6019/CHEMBL5060014 Aurora kinase A 1
- 10.6019/CHEMBL5060014 Bromodomain-containing protein 4 1
- 10.6019/CHEMBL5060014 Peregrin 1
- 10.6019/CHEMBL5060014 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL5060014 Casein kinase I isoform delta 1
- 10.6019/CHEMBL5060014 Fibroblast growth factor receptor 3 1
- 10.6019/CHEMBL5060014 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL5060014 Mitogen-activated protein kinase 1 1
- 10.6019/CHEMBL5060014 Transcription intermediary factor 1-alpha 1

Data from ChEMBL 36 via Core Engine