General Information
ZINC ID ZINC000068106869
Molecular Weight (Da)407
SMILESCS(=O)(=O)N1CCc2c(cc(-c3cccc(Cl)c3)c(=O)n2CC2CCC2)C1
Molecular FormulaC20Cl1N2O3S1
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity107.102
HBA3
HBD0
Rotatable Bonds4
Heavy Atoms27
LogP3.67
Activity (Ki) in nM100
Polar Surface Area (PSA)67.76
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 binding0.80970472
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms12
Fraction csp30.45
Ilogp3.31
Xlogp32.62
Wlogp3.83
Mlogp2.79
Silicos-it log p3.4
Consensus log p3.19
Esol log s-4.08
Esol solubility (mg/ml)3.40E-02
Esol solubility (mol/l)8.35E-05
Esol classModerately
Ali log s-3.69
Ali solubility (mg/ml)8.25E-02
Ali solubility (mol/l)2.03E-04
Ali classSoluble
Silicos-it logsw-5.92
Silicos-it solubility (mg/ml)4.91E-04
Silicos-it solubility (mol/l)1.21E-06
Silicos-it classModerately soluble
Pgp substrate
Log kp (cm/s)-6.92
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 violations1
Synthetic accessibility3.38
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-5.81
Logd3.541
Logp4.274
F (20%)0.003
F (30%)0.035
Mdck2.59E-05
Ppb0.9466
Vdss0.478
Fu0.0418
Cyp1a2-inh0.808
Cyp1a2-sub0.684
Cyp2c19-inh0.9
Cyp2c19-sub0.136
Cl6.51
T120.057
H-ht0.924
Dili0.887
Roa0.156
Fdamdd0.903
Skinsen0.033
Ec0.003
Ei0.013
Respiratory0.32
Bcf2.487
Igc504.852
Lc506.018
Lc50dm5.539
Nr-ar0.003
Nr-ar-lbd0.003
Nr-ahr0.532
Nr-aromatase0.854
Nr-er0.082
Nr-er-lbd0.032
Nr-ppar-gamma0.149
Sr-are0.7
Sr-atad50.006
Sr-hse0.83
Sr-mmp0.416
Sr-p530.653
Vol386.516
Dense1.051
Flex24
Nstereo0.167
Nongenotoxic carcinogenicity0
Ld50 oral1
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization2
Acute aquatic toxicity0
Toxicophores1
Qed0
Synth0.782
Fsp32.567
Mce-180.45
Natural product-likeness59.586
Alarm nmr-1.402
Bms1
Chelating0
Pfizer0
GskRejected
GoldentriangleRejected