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Compound Detail

CHEMBL2177238

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CN1C(=O)N(c2ccc(C#N)c(C(F)(F)F)c2)C(=O)[C@@]1(C)c1ccc(O)cc1

Basic Information

ChEMBL ID CHEMBL2177238
Phase Preclinical
Structure Type MOL
InChI Key IHPVXUVRRPAUIQ-GOSISDBHSA-N
2
Targets
3
Activities
2
Assay Types
2
PK Parameters
8
Publications
0
Known Names

Molecular Properties

389.3
MW (Da)
3.60
ALogP
4
HBA
1
HBD
84.6
PSA (Ų)
0.80
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H14F3N3O3
MW 389.33
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.94

Activity Summary

IC50 2 meas. best 8.02
EC50 1 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
EC50 9.05 9.05 0.9 1
Androgen receptor
CHEMBL1871
IC50 8.02 8.02 9.6 1
Progesterone receptor
CHEMBL208
IC50 5.06 5.06 8800.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 9.0 % Macaca mulatta
F 9.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22897611 10.1021/jm300249m Rattus norvegicus 13
22957947 10.1021/jm300281x Rattus norvegicus 4
22897611 10.1021/jm300249m Androgen receptor 3
22897611 10.1021/jm300249m Glucocorticoid receptor 1
22897611 10.1021/jm300249m Estrogen receptor 1
22897611 10.1021/jm300249m Progesterone receptor 1
22957947 10.1021/jm300281x Rhesus monkey 1
35063736 10.1016/j.ejmech.2022.114119 Androgen receptor 1

Data from ChEMBL 36 via Core Engine