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Compound Detail

CHEMBL24955

BEXLOSTERIDE
🧪 Phase II
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🧪 Phase II
CN1C(=O)CC[C@@H]2c3ccc(Cl)cc3CC[C@H]21

Basic Information

ChEMBL ID CHEMBL24955
Name BEXLOSTERIDE
Phase Phase II
Structure Type MOL
InChI Key WQBIOEFDDDEARX-CHWSQXEVSA-N

Known Names

Bexlosterida Bexlosteride LY-191704 LY-300502 LY300502
4
Targets
15
Activities
2
Assay Types
0
PK Parameters
15
Publications
5
Known Names

Molecular Properties

249.7
MW (Da)
2.99
ALogP
1
HBA
0
HBD
20.3
PSA (Ų)
0.69
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -ster-; -steride
USAN Year 1998

Extended Properties

Molecular Formula C14H16ClNO
MW 249.74
Aromatic Rings 1
Heavy Atoms 17
NP-Likeness 0.26

Activity Summary

IC50 9 meas. best 8.64
Ki 6 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
3-oxo-5-alpha-steroid 4-dehydrogenase 1
CHEMBL1787
IC50 8.64 8.196 2.3 5
3-oxo-5-alpha-steroid 4-dehydrogenase 1
CHEMBL1787
Ki 8.4 8.31 4.0 2
3-oxo-5-alpha-steroid 4-dehydrogenase 1
CHEMBL3422
Ki 8.1 8.1 8.0 1
3-oxo-5-alpha-steroid 4-dehydrogenase 2
CHEMBL1856
Ki 6.0 5.96 1000.0 2
3-oxo-5-alpha-steroid 4-dehydrogenase 2
CHEMBL1856
IC50 5.76 5.38 1750.0 4
3-oxo-5-alpha-steroid 4-dehydrogenase 2
CHEMBL5099
Ki 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
3-oxo-5-alpha-steroid 4-dehydrogenase 1 IC50 = 2.3 nM 8.64 Inhibitory activity against Steroid 5-alpha-reductase type I in human scalp homo... 11020287
3-oxo-5-alpha-steroid 4-dehydrogenase 1 Ki = 4.0 nM 8.4 In vitro inhibition of recombinant human Steroid 5-alpha-reductase type I -
3-oxo-5-alpha-steroid 4-dehydrogenase 1 Ki = 6.0 nM 8.22 In vitro inhibition of recombinant human Steroid 5-alpha-reductase type I -
3-oxo-5-alpha-steroid 4-dehydrogenase 1 IC50 = 8.0 nM 8.1 In vitro inhibition of DHT production in Hs 68 (human genital fibroblast) cells. 8381185
3-oxo-5-alpha-steroid 4-dehydrogenase 1 IC50 = 8.0 nM 8.1 Inhibition of human Steroid 5-alpha-reductase type I 10714498
3-oxo-5-alpha-steroid 4-dehydrogenase 1 Ki = 8.0 nM 8.1 Binding affinity on rat 5-alpha reductase-1 isozyme 9135028
3-oxo-5-alpha-steroid 4-dehydrogenase 1 IC50 = 8.6 nM 8.07 Inhibition of recombinant human Steroid 5-alpha-reductase type I 7650670
3-oxo-5-alpha-steroid 4-dehydrogenase 1 IC50 = 8.6 nM 8.07 Inhibition of type 1 steroid-5-alpha-reductase 7966146
3-oxo-5-alpha-steroid 4-dehydrogenase 2 Ki = 1000.0 nM 6.0 In vitro inhibition of recombinant human Steroid 5-alpha-reductase type 2 -
3-oxo-5-alpha-steroid 4-dehydrogenase 2 Ki = 1200.0 nM 5.92 In vitro inhibition of recombinant human Steroid 5-alpha-reductase type 2 -
3-oxo-5-alpha-steroid 4-dehydrogenase 2 IC50 = 1750.0 nM 5.76 Inhibition of recombinant human Steroid 5-alpha-reductase type 2 7650670
3-oxo-5-alpha-steroid 4-dehydrogenase 2 IC50 = 1750.0 nM 5.76 Inhibition of type 2 steroid-5-alpha-reductase 7966146
3-oxo-5-alpha-steroid 4-dehydrogenase 2 IC50 = 10000.0 nM 5.0 Compound was tested for inhibition of Type II 5-alpha-reductase in Human Prostat... 8381185
3-oxo-5-alpha-steroid 4-dehydrogenase 2 IC50 = 10000.0 nM 5.0 Compound was tested for inhibition against human Steroid 5-alpha-reductase type ... 10714498
3-oxo-5-alpha-steroid 4-dehydrogenase 2 Ki = 10000.0 nM 5.0 Binding affinity on rat 5-alpha reductase-2 isozyme 9135028

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(01)80363-2 3-oxo-5-alpha-steroid 4-dehydrogenase 1 2
- 10.1016/S0960-894X(01)80363-2 3-oxo-5-alpha-steroid 4-dehydrogenase 2 2
9135028 10.1021/jm960697s 3-oxo-5-alpha-steroid 4-dehydrogenase 1 1
9135028 10.1021/jm960697s 3-oxo-5-alpha-steroid 4-dehydrogenase 2 1
8381185 10.1021/jm00055a014 3-oxo-5-alpha-steroid 4-dehydrogenase 1 1
8381185 10.1021/jm00055a014 3-oxo-5-alpha-steroid 4-dehydrogenase 2 1
10714498 10.1016/s0960-894x(99)00698-8 3-oxo-5-alpha-steroid 4-dehydrogenase 1 1
10714498 10.1016/s0960-894x(99)00698-8 3-oxo-5-alpha-steroid 4-dehydrogenase 2 1
- 10.1016/0960-894X(96)00136-9 3-oxo-5-alpha-steroid 4-dehydrogenase 1 1
11020287 10.1021/jm000945r 3-oxo-5-alpha-steroid 4-dehydrogenase 1 1
11020287 10.1021/jm000945r 3-oxo-5-alpha-steroid 4-dehydrogenase 2 1
7650670 10.1021/jm00017a001 3-oxo-5-alpha-steroid 4-dehydrogenase 1 1
7650670 10.1021/jm00017a001 3-oxo-5-alpha-steroid 4-dehydrogenase 2 1
7966146 10.1021/jm00049a003 3-oxo-5-alpha-steroid 4-dehydrogenase 1 1
7966146 10.1021/jm00049a003 3-oxo-5-alpha-steroid 4-dehydrogenase 2 1

Data from ChEMBL 36 via Core Engine