General Information
ZINC ID ZINC000043078768
Molecular Weight (Da)370
SMILESCOCCS(=O)(=O)N1CCc2c(nc(CC(C)(C)C)n2CC2CC2)C1
Molecular FormulaC18N3O3S1
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity98.431
HBA4
HBD0
Rotatable Bonds8
Heavy Atoms25
LogP1.828
Activity (Ki) in nM21.38
Polar Surface Area (PSA)72.81
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 binding0.25196504
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms5
Fraction csp30.83
Ilogp3.2
Xlogp31.76
Wlogp2.7
Mlogp0.98
Silicos-it log p2.35
Consensus log p2.2
Esol log s-2.86
Esol solubility (mg/ml)5.10E-01
Esol solubility (mol/l)1.38E-03
Esol classSoluble
Ali log s-2.91
Ali solubility (mg/ml)4.58E-01
Ali solubility (mol/l)1.24E-03
Ali classSoluble
Silicos-it logsw-4
Silicos-it solubility (mg/ml)3.65E-02
Silicos-it solubility (mol/l)9.89E-05
Silicos-it classModerately soluble
Pgp substrate
Log kp (cm/s)-7.3
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 violations2
Synthetic accessibility3.83
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-2.902
Logd2.311
Logp2.288
F (20%)0.585
F (30%)0.175
Mdck2.82E-05
Ppb0.7343
Vdss2.375
Fu0.3545
Cyp1a2-inh0.028
Cyp1a2-sub0.114
Cyp2c19-inh0.645
Cyp2c19-sub0.707
Cl8.078
T120.671
H-ht0.934
Dili0.517
Roa0.307
Fdamdd0.898
Skinsen0.069
Ec0.003
Ei0.01
Respiratory0.837
Bcf1.358
Igc502.716
Lc504.201
Lc50dm3.97
Nr-ar0.001
Nr-ar-lbd0.004
Nr-ahr0.072
Nr-aromatase0.952
Nr-er0.069
Nr-er-lbd0.599
Nr-ppar-gamma0.098
Sr-are0.521
Sr-atad50.002
Sr-hse0.45
Sr-mmp0.025
Sr-p530.423
Vol366.812
Dense1.007
Flex15
Nstereo0.533
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization2
Acute aquatic toxicity0
Toxicophores0
Qed1
Synth0.739
Fsp33.017
Mce-180.833
Natural product-likeness49.636
Alarm nmr-1.338
Bms1
Chelating0
Pfizer0
GskAccepted
GoldentriangleAccepted