General Information
ZINC ID ZINC000044351483
Molecular Weight (Da)295
SMILESCCCCCCCCC/C=C/C=C/C(=O)NCC(C)(C)O
Molecular FormulaC18N1O2
ActionAntagonist
Chemical Structure
Physicochemical Details
Molar Refractivity92.159
HBA2
HBD2
Rotatable Bonds12
Heavy Atoms21
LogP4.527
Activity (Ki) in nM4570.88
Polar Surface Area (PSA)49.33
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 binding0.47792154
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms0
Fraction csp30.72
Ilogp4.22
Xlogp35.16
Wlogp4.13
Mlogp3.18
Silicos-it log p4.71
Consensus log p4.28
Esol log s-4.06
Esol solubility (mg/ml)0.0255
Esol solubility (mol/l)0.0000862
Esol classModerately
Ali log s-5.94
Ali solubility (mg/ml)0.000338
Ali solubility (mol/l)0.00000114
Ali classModerately
Silicos-it logsw-4.33
Silicos-it solubility (mg/ml)0.0138
Silicos-it solubility (mol/l)0.0000468
Silicos-it classModerately soluble
Pgp substrate
Log kp (cm/s)-4.44
Lipinski number of violations0
Ghose number of violations0
Veber number of violations1
Egan number of violations0
Muegge number of violations1
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts2
Leadlikeness number of violations2
Synthetic accessibility3.44
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-3.334
Logd3.645
Logp4.006
F (20%)0.012
F (30%)0.007
Mdck-
Ppb94.92%
Vdss0.732
Fu4.45%
Cyp1a2-inh0.23
Cyp1a2-sub0.408
Cyp2c19-inh0.694
Cyp2c19-sub0.72
Cl6.935
T120.515
H-ht0.248
Dili0.012
Roa0.629
Fdamdd0.887
Skinsen0.967
Ec0.049
Ei0.196
Respiratory0.872
Bcf0.407
Igc503.961
Lc503.752
Lc50dm3.989
Nr-ar0.006
Nr-ar-lbd0.002
Nr-ahr0.024
Nr-aromatase0.053
Nr-er0.106
Nr-er-lbd0.004
Nr-ppar-gamma0.006
Sr-are0.448
Sr-atad50.004
Sr-hse0.815
Sr-mmp0.19
Sr-p530.972
Vol340.552
Dense0.867
Flex4.333
Nstereo0
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl1
Nonbiodegradable0
Skin sensitization0
Acute aquatic toxicity-
Toxicophores1
Qed0.42
Synth2.697
Fsp30.722
Mce-180
Natural product-likeness1.087
Alarm nmr0
Bms0
Chelating0
Pfizer-
GskRejected
GoldentriangleAccepted