General Information
ZINC ID ZINC000040934591
Molecular Weight (Da)382
SMILESCSC(=S)N1CC2(CCCCC2)CO/C1=Nc1cc(C(C)(C)C)no1
Molecular FormulaC18N3O2S2
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity104.762
HBA5
HBD0
Rotatable Bonds4
Heavy Atoms25
LogP6.317
Activity (Ki) in nM1
Polar Surface Area (PSA)108.25
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 binding0.725
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms5
Fraction csp30.72
Ilogp3.77
Xlogp35.78
Wlogp4.51
Mlogp3.28
Silicos-it log p5.01
Consensus log p4.47
Esol log s-5.73
Esol solubility (mg/ml)0.000709
Esol solubility (mol/l)0.00000186
Esol classModerately
Ali log s-7.82
Ali solubility (mg/ml)0.00000574
Ali solubility (mol/l)1.51E-08
Ali classPoorly sol
Silicos-it logsw-4.63
Silicos-it solubility (mg/ml)0.0089
Silicos-it solubility (mol/l)0.0000233
Silicos-it classModerately soluble
Pgp substrate
Log kp (cm/s)-4.52
Lipinski number of violations0
Ghose number of violations0
Veber number of violations0
Egan number of violations0
Muegge number of violations1
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts2
Leadlikeness number of violations2
Synthetic accessibility4.81
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-5.393
Logd4.415
Logp4.926
F (20%)0.001
F (30%)0.005
Mdck1.20E-05
Ppb0.9817
Vdss1.524
Fu0.0196
Cyp1a2-inh0.834
Cyp1a2-sub0.728
Cyp2c19-inh0.889
Cyp2c19-sub0.783
Cl1.356
T120.035
H-ht0.76
Dili0.908
Roa0.214
Fdamdd0.917
Skinsen0.042
Ec0.004
Ei0.052
Respiratory0.971
Bcf2.896
Igc505.046
Lc506.565
Lc50dm5.111
Nr-ar0.013
Nr-ar-lbd0.011
Nr-ahr0.969
Nr-aromatase0.832
Nr-er0.583
Nr-er-lbd0.077
Nr-ppar-gamma0.907
Sr-are0.942
Sr-atad50.393
Sr-hse0.969
Sr-mmp0.968
Sr-p530.521
Vol371.258
Dense1.027
Flex0.211
Nstereo0
Nongenotoxic carcinogenicity2
Ld50 oral0
Genotoxic carcinogenicity mutagenicity1
Surechembl4
Nonbiodegradable2
Skin sensitization4
Acute aquatic toxicity1
Toxicophores3
Qed0.646
Synth4.139
Fsp30.722
Mce-1870.323
Natural product-likeness-0.515
Alarm nmr1
Bms0
Chelating0
Pfizer1
GskRejected
GoldentriangleAccepted