General Information
ZINC ID ZINC000045357416
Molecular Weight (Da)392
SMILESCCCCCc1cc(NS(C)(=O)=O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=C[C@@H]21
Molecular FormulaC22N1O3S1
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity111.806
HBA3
HBD1
Rotatable Bonds6
Heavy Atoms27
LogP5.263
Activity (Ki) in nM1737.801
Polar Surface Area (PSA)63.78
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 binding0.83902978
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms6
Fraction csp30.64
Ilogp3.93
Xlogp36.29
Wlogp6.29
Mlogp3.53
Silicos-it log p4.48
Consensus log p4.9
Esol log s-6
Esol solubility (mg/ml)3.93E-04
Esol solubility (mol/l)1.00E-06
Esol classModerately
Ali log s-7.42
Ali solubility (mg/ml)1.50E-05
Ali solubility (mol/l)3.82E-08
Ali classPoorly sol
Silicos-it logsw-6.82
Silicos-it solubility (mg/ml)5.97E-05
Silicos-it solubility (mol/l)1.52E-07
Silicos-it classPoorly soluble
Pgp substrate
Log kp (cm/s)-4.22
Lipinski number of violations0
Ghose number of violations1
Veber number of violations0
Egan number of violations1
Muegge number of violations1
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts1
Leadlikeness number of violations2
Synthetic accessibility4.52
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-2.68
Logd3.384
Logp6.14
F (20%)0.997
F (30%)0.98
Mdck2.14E-05
Ppb1.0043
Vdss1.5
Fu0.0199
Cyp1a2-inh0.605
Cyp1a2-sub0.793
Cyp2c19-inh0.954
Cyp2c19-sub0.855
Cl2.817
T120.137
H-ht0.968
Dili0.842
Roa0.197
Fdamdd0.945
Skinsen0.107
Ec0.003
Ei0.013
Respiratory0.78
Bcf2.241
Igc504.653
Lc506.742
Lc50dm6.535
Nr-ar0.532
Nr-ar-lbd0.005
Nr-ahr0.319
Nr-aromatase0.014
Nr-er0.041
Nr-er-lbd0.005
Nr-ppar-gamma0.195
Sr-are0.346
Sr-atad50.003
Sr-hse0.017
Sr-mmp0.804
Sr-p530.032
Vol408.729
Dense0.957
Flex18
Nstereo0.333
Nongenotoxic carcinogenicity2
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl1
Nonbiodegradable0
Skin sensitization0
Acute aquatic toxicity2
Toxicophores0
Qed1
Synth0.522
Fsp33.581
Mce-180.636
Natural product-likeness72.111
Alarm nmr1.2
Bms2
Chelating0
Pfizer2
GskRejected
GoldentriangleRejected