General Information
ZINC ID ZINC000040952361
Molecular Weight (Da)420
SMILESCC(C)CCOc1cc(O)cc(OCCCCCCCCCCC(=O)NC2CC2)c1
Molecular FormulaC25N1O4
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity120.775
HBA4
HBD2
Rotatable Bonds17
Heavy Atoms30
LogP6.423
Activity (Ki) in nM125.893
Polar Surface Area (PSA)67.79
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
+
Biodegradation0
Glucocorticoid receptor binding+
Thyroid receptor binding+
Androgen receptor binding-
Plasma protein binding1.08083975
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms6
Fraction csp30.72
Ilogp4.99
Xlogp36.78
Wlogp5.92
Mlogp3.36
Silicos-it log p6.45
Consensus log p5.5
Esol log s-5.67
Esol solubility (mg/ml)0.000891
Esol solubility (mol/l)0.00000212
Esol classModerately
Ali log s-8.01
Ali solubility (mg/ml)0.0000041
Ali solubility (mol/l)9.76E-09
Ali classPoorly sol
Silicos-it logsw-7.49
Silicos-it solubility (mg/ml)0.0000136
Silicos-it solubility (mol/l)3.25E-08
Silicos-it classPoorly soluble
Pgp substrate
Log kp (cm/s)-4.05
Lipinski number of violations0
Ghose number of violations2
Veber number of violations1
Egan number of violations1
Muegge number of violations2
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts0
Leadlikeness number of violations3
Synthetic accessibility3.26
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-4.814
Logd4.548
Logp6.381
F (20%)0.995
F (30%)0.993
Mdck2.55E-05
Ppb0.9856
Vdss0.818
Fu0.0189
Cyp1a2-inh0.289
Cyp1a2-sub0.261
Cyp2c19-inh0.831
Cyp2c19-sub0.122
Cl9.72
T120.271
H-ht0.257
Dili0.062
Roa0.12
Fdamdd0.28
Skinsen0.944
Ec0.003
Ei0.043
Respiratory0.154
Bcf0.975
Igc505.142
Lc504.833
Lc50dm5.092
Nr-ar0.045
Nr-ar-lbd0.003
Nr-ahr0.839
Nr-aromatase0.392
Nr-er0.865
Nr-er-lbd0.013
Nr-ppar-gamma0.139
Sr-are0.76
Sr-atad50.198
Sr-hse0.671
Sr-mmp0.938
Sr-p530.439
Vol459.455
Dense0.913
Flex1.8
Nstereo0
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization1
Acute aquatic toxicity0
Toxicophores2
Qed0.305
Synth2.3
Fsp30.72
Mce-1825.674
Natural product-likeness-0.236
Alarm nmr1
Bms1
Chelating0
Pfizer0
GskRejected
GoldentriangleAccepted