General Information
ZINC ID ZINC000043199856
Molecular Weight (Da)392
SMILESCCS(=O)(=O)c1ccc2c(c1)nc(C(C)(C)C)n2CC1CCN(C=O)CC1
Molecular FormulaC20N3O3S1
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity106.192
HBA4
HBD0
Rotatable Bonds5
Heavy Atoms27
LogP3.582
Activity (Ki) in nM22.909
Polar Surface Area (PSA)80.65
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 binding0.39239817
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms9
Fraction csp30.6
Ilogp2.76
Xlogp32.94
Wlogp3.7
Mlogp2.77
Silicos-it log p2.65
Consensus log p2.96
Esol log s-3.97
Esol solubility (mg/ml)4.19E-02
Esol solubility (mol/l)1.07E-04
Esol classSoluble
Ali log s-4.3
Ali solubility (mg/ml)1.98E-02
Ali solubility (mol/l)5.06E-05
Ali classModerately
Silicos-it logsw-4.79
Silicos-it solubility (mg/ml)6.35E-03
Silicos-it solubility (mol/l)1.62E-05
Silicos-it classModerately soluble
Pgp substrate
Log kp (cm/s)-6.6
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 alerts1
Leadlikeness number of violations1
Synthetic accessibility3.17
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-2.559
Logd2.014
Logp2.256
F (20%)0.007
F (30%)0.007
Mdck2.55E-05
Ppb0.4995
Vdss1.599
Fu0.6299
Cyp1a2-inh0.123
Cyp1a2-sub0.802
Cyp2c19-inh0.584
Cyp2c19-sub0.724
Cl3.039
T120.101
H-ht0.684
Dili0.397
Roa0.376
Fdamdd0.932
Skinsen0.04
Ec0.003
Ei0.012
Respiratory0.615
Bcf0.542
Igc502.553
Lc503.717
Lc50dm3.793
Nr-ar0.015
Nr-ar-lbd0.008
Nr-ahr0.053
Nr-aromatase0.011
Nr-er0.147
Nr-er-lbd0.25
Nr-ppar-gamma0.007
Sr-are0.496
Sr-atad50.003
Sr-hse0.027
Sr-mmp0.189
Sr-p530.017
Vol393.494
Dense0.994
Flex19
Nstereo0.316
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable1
Skin sensitization1
Acute aquatic toxicity1
Toxicophores0
Qed4
Synth0.735
Fsp32.769
Mce-180.6
Natural product-likeness50.875
Alarm nmr-1.634
Bms2
Chelating0
Pfizer1
GskAccepted
GoldentriangleAccepted