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Compound Detail

CHEMBL4758064

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CC[C@H]1[C@@H](O)[C@@H]2[C@H]([C@@H](O)C[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@@H]23)[C@@]2(C)CC[C@@H](O)C[C@@H]12

Basic Information

ChEMBL ID CHEMBL4758064
Phase Preclinical
Structure Type MOL
InChI Key UEXTVLKDFZEPMH-PAEMJXPASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
19
Publications
0
Known Names

Molecular Properties

436.6
MW (Da)
4.08
ALogP
4
HBA
4
HBD
98.0
PSA (Ų)
0.52
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H44O5
MW 436.63
Aromatic Rings 0
Heavy Atoms 31
NP-Likeness 2.60

Activity Summary

EC50 1 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile acid receptor
CHEMBL2047
EC50 6.85 6.85 140.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bile acid receptor EC50 = 140.0 nM 6.85 Agonist activity at glutathione transferase-tagged human FXR-LBD using biotinyla... 27652492

Literature References

PubMed DOI Target Context # Activities
27652492 10.1021/acs.jmedchem.6b01126 ADMET 13
27652492 10.1021/acs.jmedchem.6b01126 Bile acid receptor 11
27652492 10.1021/acs.jmedchem.6b01126 No relevant target 3
27652492 10.1021/acs.jmedchem.6b01126 Unchecked 3
27652492 10.1021/acs.jmedchem.6b01126 HepG2 2
27652492 10.1021/acs.jmedchem.6b01126 Retinoic acid receptor RXR-alpha 1
27652492 10.1021/acs.jmedchem.6b01126 Albumin 1
27652492 10.1021/acs.jmedchem.6b01126 Glucocorticoid receptor 1
27652492 10.1021/acs.jmedchem.6b01126 Thyroid hormone receptor alpha 1
27652492 10.1021/acs.jmedchem.6b01126 Progesterone receptor 1
27652492 10.1021/acs.jmedchem.6b01126 Estrogen receptor 1
27652492 10.1021/acs.jmedchem.6b01126 Vitamin D3 receptor 1
27652492 10.1021/acs.jmedchem.6b01126 Nuclear receptor subfamily 1 group I member 2 1
27652492 10.1021/acs.jmedchem.6b01126 Peroxisome proliferator-activated receptor gamma 1
27652492 10.1021/acs.jmedchem.6b01126 Peroxisome proliferator-activated receptor delta 1
27652492 10.1021/acs.jmedchem.6b01126 Peroxisome proliferator-activated receptor alpha 1
27652492 10.1021/acs.jmedchem.6b01126 Oxysterols receptor LXR-beta 1
27652492 10.1021/acs.jmedchem.6b01126 Nuclear receptor subfamily 1 group I member 3 1
27652492 10.1021/acs.jmedchem.6b01126 G-protein coupled bile acid receptor 1 1

Data from ChEMBL 36 via Core Engine