General Information
ZINC ID ZINC000299822353
Molecular Weight (Da)377
SMILESCC(C)(C)c1cc(NC(=O)[C@@H]2CCCCN2C(=O)[C@@H]2CC[C@@H](O)CC2)no1
Molecular FormulaC20N3O4
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity99.362
HBA5
HBD2
Rotatable Bonds4
Heavy Atoms27
LogP2.801
Activity (Ki) in nM40.738
Polar Surface Area (PSA)95.67
Chemical Structure
Pharmacokinetic Properties (AdmetSAR)
Human intestinal absorption+
Caco-2-
Blood brain barrier-
P-glycoprotein inhibitior-
P-glycoprotein substrate-
Cyp3a4 substrate+
Cyp2c9 substrate-
Cyp2d6 substrate-
Cyp3a4 inhibition-
Cyp2c9 inhibition-
Cyp2c19 inhibition-
Cyp2d6 inhibition-
Cyp1a2 inhibition-
Acute oral toxicity-
Carcinogenicity (binary)-
Ames mutagenesis-
Human ether-a-go-go-related
gene inhibition
-
Biodegradation
Glucocorticoid receptor binding+
Thyroid receptor binding+
Androgen receptor binding+
Plasma protein binding0.5806548
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms5
Fraction csp30.75
Ilogp2.54
Xlogp32.55
Wlogp2.27
Mlogp1.31
Silicos-it log p2.05
Consensus log p2.15
Esol log s-3.53
Esol solubility (mg/ml)1.12E-01
Esol solubility (mol/l)2.97E-04
Esol classSoluble
Ali log s-4.21
Ali solubility (mg/ml)2.35E-02
Ali solubility (mol/l)6.22E-05
Ali classModerately
Silicos-it logsw-3.46
Silicos-it solubility (mg/ml)1.30E-01
Silicos-it solubility (mol/l)3.44E-04
Silicos-it classSoluble
Pgp substrate
Log kp (cm/s)-6.79
Lipinski number of violations0
Ghose number of violations0
Veber number of violations0
Egan number of violations0
Muegge number of violations0
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts0
Leadlikeness number of violations1
Synthetic accessibility4.46
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-3.375
Logd2.075
Logp2.165
F (20%)0.003
F (30%)0.021
Mdck1.03E-05
Ppb0.9026
Vdss0.693
Fu0.1097
Cyp1a2-inh0.031
Cyp1a2-sub0.689
Cyp2c19-inh0.595
Cyp2c19-sub0.408
Cl3.394
T120.721
H-ht0.982
Dili0.926
Roa0.961
Fdamdd0.651
Skinsen0.183
Ec0.003
Ei0.011
Respiratory0.914
Bcf0.625
Igc502.722
Lc502.972
Lc50dm4.422
Nr-ar0.403
Nr-ar-lbd0.003
Nr-ahr0.017
Nr-aromatase0.383
Nr-er0.227
Nr-er-lbd0.007
Nr-ppar-gamma0.09
Sr-are0.524
Sr-atad50.003
Sr-hse0.428
Sr-mmp0.305
Sr-p530.056
Vol386.412
Dense0.976
Flex20
Nstereo0.25
Nongenotoxic carcinogenicity1
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization1
Acute aquatic toxicity1
Toxicophores0
Qed0
Synth0.826
Fsp33.707
Mce-180.75
Natural product-likeness72.571
Alarm nmr-0.67
Bms2
Chelating0
Pfizer1
GskAccepted
GoldentriangleAccepted