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Compound Detail

CHEMBL3084690

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Cc1c(N2[C@@H]3CC[C@H]2C[C@@H](O)C3)ccc(C#N)c1Cl

Basic Information

ChEMBL ID CHEMBL3084690
Phase Preclinical
Structure Type MOL
InChI Key KRPAAKPHVZQMIF-ITGUQSILSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

276.8
MW (Da)
3.01
ALogP
3
HBA
1
HBD
47.3
PSA (Ų)
0.86
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H17ClN2O
MW 276.77
Aromatic Rings 1
Heavy Atoms 19
NP-Likeness -0.28

Activity Summary

EC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL3056
EC50 8.7 8.7 2.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 214.0 uL/ml.millig Rattus norvegicus
CL 69.0 uL/ml.millig Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Androgen receptor EC50 = 1.995 nM 8.7 Agonist activity at androgen receptor in mouse NIH3T3 cells transiently transfec... 19856921

Literature References

PubMed DOI Target Context # Activities
19856921 10.1021/jm901149c Androgen receptor 2
19856921 10.1021/jm901149c Liver microsomes 2

Data from ChEMBL 36 via Core Engine