General Information
ZINC ID ZINC000169313063
Molecular Weight (Da)390
SMILESO=C(NC1(c2ccccn2)CCC1)C1=NN(c2c[n+]([O-])ccn2)[C@H]2[C@H]3C[C@H]3C[C@@H]12
Molecular FormulaC21N6O2
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity102.824
HBA4
HBD1
Rotatable Bonds4
Heavy Atoms29
LogP-0.958
Activity (Ki) in nM32.359
Polar Surface Area (PSA)97.42
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 binding0.72585237
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms12
Fraction csp30.48
Ilogp1.83
Xlogp30.46
Wlogp0.64
Mlogp1.54
Silicos-it log p0.93
Consensus log p1.08
Esol log s-2.53
Esol solubility (mg/ml)1.16E+00
Esol solubility (mol/l)2.97E-03
Esol classSoluble
Ali log s-2.04
Ali solubility (mg/ml)3.53E+00
Ali solubility (mol/l)9.05E-03
Ali classSoluble
Silicos-it logsw-3.81
Silicos-it solubility (mg/ml)6.09E-02
Silicos-it solubility (mol/l)1.56E-04
Silicos-it classSoluble
Pgp substrate
Log kp (cm/s)-8.36
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 alerts2
Leadlikeness number of violations1
Synthetic accessibility4.93
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-3.193
Logd2.048
Logp1.325
F (20%)0.07
F (30%)0.017
Mdck1.62E-05
Ppb0.5145
Vdss1.334
Fu0.4647
Cyp1a2-inh0.032
Cyp1a2-sub0.572
Cyp2c19-inh0.069
Cyp2c19-sub0.159
Cl3.737
T120.441
H-ht0.625
Dili0.49
Roa0.12
Fdamdd0.928
Skinsen0.804
Ec0.003
Ei0.009
Respiratory0.945
Bcf0.389
Igc502.015
Lc502.389
Lc50dm3.208
Nr-ar0.018
Nr-ar-lbd0.034
Nr-ahr0.36
Nr-aromatase0.626
Nr-er0.103
Nr-er-lbd0.008
Nr-ppar-gamma0.008
Sr-are0.442
Sr-atad50.021
Sr-hse0.007
Sr-mmp0.322
Sr-p530.544
Vol382.903
Dense1.019
Flex27
Nstereo0.185
Nongenotoxic carcinogenicity3
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization1
Acute aquatic toxicity0
Toxicophores0
Qed1
Synth0.39
Fsp34.62
Mce-180.429
Natural product-likeness109.533
Alarm nmr-0.465
Bms1
Chelating1
Pfizer0
GskAccepted
GoldentriangleAccepted