General Information
ZINC ID ZINC000045291465
Molecular Weight (Da)330
SMILESCc1ccc(NC(=O)[C@H]2CCCC[C@@H]2C)cc1CN1CCOCC1
Molecular FormulaC20N2O2
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity97.549
HBA2
HBD1
Rotatable Bonds4
Heavy Atoms24
LogP3.576
Activity (Ki) in nM1584.89
Polar Surface Area (PSA)41.57
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 binding0.83342379
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms6
Fraction csp30.65
Ilogp3.67
Xlogp33.44
Wlogp2.87
Mlogp2.58
Silicos-it log p3.63
Consensus log p3.24
Esol log s-3.91
Esol solubility (mg/ml)0.0406
Esol solubility (mol/l)0.000123
Esol classSoluble
Ali log s-3.99
Ali solubility (mg/ml)0.0335
Ali solubility (mol/l)0.000101
Ali classSoluble
Silicos-it logsw-4.94
Silicos-it solubility (mg/ml)0.00378
Silicos-it solubility (mol/l)0.0000114
Silicos-it classModerately soluble
Pgp substrate
Log kp (cm/s)-5.87
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 violations0
Synthetic accessibility3.26
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-3.874
Logd3.791
Logp4.028
F (20%)0.233
F (30%)0.017
Mdck-
Ppb93.75%
Vdss1.243
Fu7.03%
Cyp1a2-inh0.185
Cyp1a2-sub0.825
Cyp2c19-inh0.833
Cyp2c19-sub0.857
Cl12.382
T120.15
H-ht0.407
Dili0.833
Roa0.617
Fdamdd0.12
Skinsen0.937
Ec0.006
Ei0.028
Respiratory0.938
Bcf0.901
Igc502.91
Lc503.81
Lc50dm4.282
Nr-ar0.068
Nr-ar-lbd0.004
Nr-ahr0.787
Nr-aromatase0.302
Nr-er0.292
Nr-er-lbd0.037
Nr-ppar-gamma0.006
Sr-are0.425
Sr-atad50.007
Sr-hse0.052
Sr-mmp0.214
Sr-p530.05
Vol357.835
Dense0.923
Flex0.263
Nstereo2
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity1
Surechembl0
Nonbiodegradable1
Skin sensitization4
Acute aquatic toxicity-
Toxicophores1
Qed0.917
Synth2.841
Fsp30.65
Mce-1857.697
Natural product-likeness-1.416
Alarm nmr0
Bms0
Chelating0
Pfizer-
GskRejected
GoldentriangleAccepted