General Information
ZINC ID ZINC000040892529
Molecular Weight (Da)398
SMILESCSC(=S)N1CC2(CCCCC2)CO/C1=Nc1nc(C(C)(C)C)cs1
Molecular FormulaC18N3O1S3
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity110.983
HBA4
HBD0
Rotatable Bonds4
Heavy Atoms25
LogP6.318
Activity (Ki) in nM1
Polar Surface Area (PSA)123.35
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 binding0.78
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms5
Fraction csp30.72
Ilogp3.82
Xlogp36.36
Wlogp4.98
Mlogp3.29
Silicos-it log p6.25
Consensus log p4.94
Esol log s-6.2
Esol solubility (mg/ml)0.000253
Esol solubility (mol/l)0.00000063
Esol classPoorly sol
Ali log s-8.74
Ali solubility (mg/ml)0.00000072
Ali solubility (mol/l)1.81E-09
Ali classPoorly sol
Silicos-it logsw-4.67
Silicos-it solubility (mg/ml)0.00842
Silicos-it solubility (mol/l)0.0000212
Silicos-it classModerately soluble
Pgp substrate
Log kp (cm/s)-4.21
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 accessibility4.71
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-6.135
Logd4.943
Logp5.969
F (20%)0.002
F (30%)0.033
Mdck1.91E-05
Ppb0.9852
Vdss1.361
Fu0.0231
Cyp1a2-inh0.922
Cyp1a2-sub0.729
Cyp2c19-inh0.896
Cyp2c19-sub0.803
Cl2.544
T120.008
H-ht0.557
Dili0.525
Roa0.149
Fdamdd0.899
Skinsen0.038
Ec0.003
Ei0.04
Respiratory0.89
Bcf2.55
Igc504.781
Lc506.549
Lc50dm5.317
Nr-ar0.009
Nr-ar-lbd0.015
Nr-ahr0.979
Nr-aromatase0.9
Nr-er0.622
Nr-er-lbd0.131
Nr-ppar-gamma0.949
Sr-are0.959
Sr-atad50.618
Sr-hse0.974
Sr-mmp0.982
Sr-p530.42
Vol380.977
Dense1.042
Flex0.211
Nstereo0
Nongenotoxic carcinogenicity2
Ld50 oral0
Genotoxic carcinogenicity mutagenicity1
Surechembl4
Nonbiodegradable2
Skin sensitization4
Acute aquatic toxicity1
Toxicophores4
Qed0.597
Synth4.051
Fsp30.722
Mce-1870.323
Natural product-likeness-0.719
Alarm nmr3
Bms0
Chelating0
Pfizer1
GskRejected
GoldentriangleAccepted