General Information
ZINC ID ZINC000071296351
Molecular Weight (Da)374
SMILESO=C(c1cccc2[nH]ccc12)N1CC[C@](O)(c2ccccc2)[C@H]2CCCC[C@@H]21
Molecular FormulaC24N2O2
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity109.194
HBA2
HBD2
Rotatable Bonds2
Heavy Atoms28
LogP3.329
Activity (Ki) in nM21.878
Polar Surface Area (PSA)56.33
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 binding0.81386536
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms15
Fraction csp30.38
Ilogp2.75
Xlogp34.02
Wlogp3.97
Mlogp3.31
Silicos-it log p4.11
Consensus log p3.63
Esol log s-4.89
Esol solubility (mg/ml)4.79E-03
Esol solubility (mol/l)1.28E-05
Esol classModerately
Ali log s-4.91
Ali solubility (mg/ml)4.65E-03
Ali solubility (mol/l)1.24E-05
Ali classModerately
Silicos-it logsw-6.48
Silicos-it solubility (mg/ml)1.25E-04
Silicos-it solubility (mol/l)3.33E-07
Silicos-it classPoorly soluble
Pgp substrate
Log kp (cm/s)-5.73
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 violations2
Synthetic accessibility3.46
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-4.683
Logd3.778
Logp3.875
F (20%)0.923
F (30%)0.012
Mdck1.46E-05
Ppb0.956
Vdss1.332
Fu0.0344
Cyp1a2-inh0.451
Cyp1a2-sub0.608
Cyp2c19-inh0.943
Cyp2c19-sub0.357
Cl2.955
T120.095
H-ht0.854
Dili0.441
Roa0.21
Fdamdd0.466
Skinsen0.942
Ec0.004
Ei0.277
Respiratory0.98
Bcf0.711
Igc504.382
Lc504.893
Lc50dm5.332
Nr-ar0.248
Nr-ar-lbd0.011
Nr-ahr0.653
Nr-aromatase0.933
Nr-er0.302
Nr-er-lbd0.022
Nr-ppar-gamma0.004
Sr-are0.336
Sr-atad50.037
Sr-hse0.179
Sr-mmp0.76
Sr-p530.142
Vol399.36
Dense0.937
Flex28
Nstereo0.107
Nongenotoxic carcinogenicity3
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization0
Acute aquatic toxicity0
Toxicophores0
Qed2
Synth0.696
Fsp33.332
Mce-180.375
Natural product-likeness92.182
Alarm nmr-0.029
Bms0
Chelating0
Pfizer0
GskRejected
GoldentriangleAccepted