General Information
ZINC ID ZINC000036294630
Molecular Weight (Da)418
SMILESCCCCCn1cc(C(=O)c2cccc3ccccc23)cc1-c1cccc2ccccc12
Molecular FormulaC30N1O1
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity130.558
HBA1
HBD0
Rotatable Bonds7
Heavy Atoms32
LogP7.718
Activity (Ki) in nM48.978
Polar Surface Area (PSA)22
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 binding1.163
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms25
Fraction csp30.17
Ilogp4.31
Xlogp37.89
Wlogp7.88
Mlogp4.91
Silicos-it log p7.6
Consensus log p6.52
Esol log s-7.52
Esol solubility (mg/ml)0.0000127
Esol solubility (mol/l)3.05E-08
Esol classPoorly sol
Ali log s-8.2
Ali solubility (mg/ml)0.00000263
Ali solubility (mol/l)6.30E-09
Ali classPoorly sol
Silicos-it logsw-11.03
Silicos-it solubility (mg/ml)3.91E-09
Silicos-it solubility (mol/l)9.38E-12
Silicos-it classInsoluble
Pgp substrate
Log kp (cm/s)-3.25
Lipinski number of violations1
Ghose number of violations2
Veber number of violations0
Egan number of violations1
Muegge number of violations1
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts0
Leadlikeness number of violations2
Synthetic accessibility3.31
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-7.384
Logd5.402
Logp7.593
F (20%)0.957
F (30%)0.971
Mdck7.76E-06
Ppb1.002
Vdss1.072
Fu0.0027
Cyp1a2-inh0.675
Cyp1a2-sub0.181
Cyp2c19-inh0.519
Cyp2c19-sub0.055
Cl4.396
T120.014
H-ht0.067
Dili0.947
Roa0.251
Fdamdd0.303
Skinsen0.647
Ec0.003
Ei0.897
Respiratory0.135
Bcf2.081
Igc505.688
Lc506.434
Lc50dm6.441
Nr-ar0.064
Nr-ar-lbd0.022
Nr-ahr0.685
Nr-aromatase0.893
Nr-er0.883
Nr-er-lbd0.751
Nr-ppar-gamma0.02
Sr-are0.9
Sr-atad50.422
Sr-hse0.181
Sr-mmp0.864
Sr-p530.276
Vol470.167
Dense0.887
Flex0.25
Nstereo0
Nongenotoxic carcinogenicity1
Ld50 oral0
Genotoxic carcinogenicity mutagenicity4
Surechembl0
Nonbiodegradable0
Skin sensitization1
Acute aquatic toxicity0
Toxicophores2
Qed0.195
Synth2.287
Fsp30.167
Mce-1825
Natural product-likeness-0.553
Alarm nmr0
Bms0
Chelating0
Pfizer0
GskRejected
GoldentriangleRejected