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Compound Detail

CHEMBL318617

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C=C1/C(=C\C=C2/CCC[C@]3(C)C([C@@H](C)CSc4ccc(C(C)(C)O)cc4)CC[C@@H]23)C[C@@H](O)C[C@@H]1O

Basic Information

ChEMBL ID CHEMBL318617
Phase Preclinical
Structure Type MOL
InChI Key IJIUMNVXKWYQCS-QLGJRHCTSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

496.8
MW (Da)
6.78
ALogP
4
HBA
3
HBD
60.7
PSA (Ų)
0.38
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 C31H44O3S
MW 496.76
Aromatic Rings 1
Heavy Atoms 35
NP-Likeness 1.75

Activity Summary

IC50 1 meas. best 9.55
Kd 1 meas. best 10.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vitamin D3 receptor
CHEMBL1977
Kd 10.05 10.05 0.1 1
Homo sapiens
CHEMBL372
IC50 9.55 9.55 0.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Vitamin D3 receptor Kd = 0.089 nM 10.05 Binding affinity to VDR receptor 11462969
Homo sapiens IC50 = 0.28 nM 9.55 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