General Information
ZINC ID ZINC000071317418
Molecular Weight (Da)358
SMILESO=C(NCC1(CO)CCCC1)c1nc(N2CCOCC2)n2ccccc12
Molecular FormulaC19N4O3
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity96.206
HBA4
HBD2
Rotatable Bonds5
Heavy Atoms26
LogP1.733
Activity (Ki) in nM33.113
Polar Surface Area (PSA)79.62
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 binding0.81796699
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms9
Fraction csp30.58
Ilogp3.28
Xlogp32.54
Wlogp1.07
Mlogp1.36
Silicos-it log p1.56
Consensus log p1.96
Esol log s-3.52
Esol solubility (mg/ml)1.08E-01
Esol solubility (mol/l)3.00E-04
Esol classSoluble
Ali log s-3.85
Ali solubility (mg/ml)5.09E-02
Ali solubility (mol/l)1.42E-04
Ali classSoluble
Silicos-it logsw-3.84
Silicos-it solubility (mg/ml)5.20E-02
Silicos-it solubility (mol/l)1.45E-04
Silicos-it classSoluble
Pgp substrate
Log kp (cm/s)-6.68
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 violations1
Synthetic accessibility2.98
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-3.641
Logd2.686
Logp2.293
F (20%)0.01
F (30%)0.013
Mdck2.58E-05
Ppb0.9037
Vdss0.932
Fu0.1217
Cyp1a2-inh0.777
Cyp1a2-sub0.205
Cyp2c19-inh0.47
Cyp2c19-sub0.385
Cl6.627
T120.203
H-ht0.921
Dili0.051
Roa0.006
Fdamdd0.948
Skinsen0.037
Ec0.003
Ei0.01
Respiratory0.291
Bcf0.256
Igc501.803
Lc502.678
Lc50dm3.553
Nr-ar0.005
Nr-ar-lbd0.003
Nr-ahr0.263
Nr-aromatase0.139
Nr-er0.124
Nr-er-lbd0.005
Nr-ppar-gamma0.005
Sr-are0.47
Sr-atad50.007
Sr-hse0.008
Sr-mmp0.06
Sr-p530.255
Vol360.13
Dense0.995
Flex22
Nstereo0.273
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl1
Nonbiodegradable0
Skin sensitization2
Acute aquatic toxicity0
Toxicophores0
Qed1
Synth0.846
Fsp32.756
Mce-180.579
Natural product-likeness54.6
Alarm nmr-1.46
Bms0
Chelating0
Pfizer0
GskAccepted
GoldentriangleAccepted