General Information
ZINC ID ZINC000058582285
Molecular Weight (Da)370
SMILESCCCCCC1=NN(C(=O)c2cccc3ccccc23)C[C@H]1c1ccccc1
Molecular FormulaC25N2O1
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity113.877
HBA2
HBD0
Rotatable Bonds6
Heavy Atoms28
LogP5.429
Activity (Ki) in nM31.6228
Polar Surface Area (PSA)32.67
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 binding1.234
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms16
Fraction csp30.28
Ilogp3.87
Xlogp36.03
Wlogp5.25
Mlogp4.8
Silicos-it log p6.1
Consensus log p5.21
Esol log s-5.9
Esol solubility (mg/ml)0.00047
Esol solubility (mol/l)0.00000127
Esol classModerately
Ali log s-6.49
Ali solubility (mg/ml)0.000119
Ali solubility (mol/l)0.00000032
Ali classPoorly sol
Silicos-it logsw-8.46
Silicos-it solubility (mg/ml)0.00000128
Silicos-it solubility (mol/l)3.47E-09
Silicos-it classPoorly soluble
Pgp substrate
Log kp (cm/s)-4.28
Lipinski number of violations1
Ghose number of violations0
Veber number of violations0
Egan number of violations0
Muegge number of violations1
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts0
Leadlikeness number of violations2
Synthetic accessibility3.9
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-6.368
Logd4.738
Logp6.162
F (20%)0.043
F (30%)0.005
Mdck-
Ppb96.27%
Vdss0.964
Fu4.21%
Cyp1a2-inh0.52
Cyp1a2-sub0.866
Cyp2c19-inh0.95
Cyp2c19-sub0.561
Cl2.316
T120.045
H-ht0.9
Dili0.959
Roa0.709
Fdamdd0.061
Skinsen0.078
Ec0.003
Ei0.018
Respiratory0.844
Bcf2.329
Igc505.117
Lc506.292
Lc50dm5.548
Nr-ar0.017
Nr-ar-lbd0.013
Nr-ahr0.432
Nr-aromatase0.389
Nr-er0.78
Nr-er-lbd0.403
Nr-ppar-gamma0.621
Sr-are0.384
Sr-atad50.009
Sr-hse0.556
Sr-mmp0.888
Sr-p530.428
Vol411.149
Dense0.9
Flex0.304
Nstereo1
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity1
Surechembl0
Nonbiodegradable0
Skin sensitization0
Acute aquatic toxicity-
Toxicophores2
Qed0.489
Synth2.816
Fsp30.28
Mce-1862.5
Natural product-likeness-0.259
Alarm nmr0
Bms0
Chelating0
Pfizer-
GskRejected
GoldentriangleAccepted