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Compound Detail

CHEMBL318267

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C=C1/C(=C\C=C2/CCC[C@]3(C)C([C@@H](C)COc4ccc(C(C)(C)O)cc4)CC[C@@H]23)C[C@@H](O)C[C@@H]1O

Basic Information

ChEMBL ID CHEMBL318267
Phase Preclinical
Structure Type MOL
InChI Key SBQPQSBIPUQYGR-QLGJRHCTSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

480.7
MW (Da)
6.07
ALogP
4
HBA
3
HBD
69.9
PSA (Ų)
0.46
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H44O4
MW 480.69
Aromatic Rings 1
Heavy Atoms 35
NP-Likeness 1.86

Activity Summary

IC50 1 meas. best 9.96
Kd 1 meas. best 10.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vitamin D3 receptor
CHEMBL1977
Kd 10.14 10.14 0.1 1
Homo sapiens
CHEMBL372
IC50 9.96 9.96 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Vitamin D3 receptor Kd = 0.073 nM 10.14 Binding affinity to VDR receptor 11462969
Homo sapiens IC50 = 0.11 nM 9.96 Inhibition of growth of human keratinocytes 11462969

Literature References

PubMed DOI Target Context # Activities
11462969 10.1021/jm0000214 Vitamin D3 receptor 1
11462969 10.1021/jm0000214 Homo sapiens 1

Data from ChEMBL 36 via Core Engine