General Information
ZINC ID ZINC000071329545
Molecular Weight (Da)393
SMILESCC(C)(C)c1cc(NC(=O)N2CCCN(C(=O)CN3CCOCC3)CC2)no1
Molecular FormulaC19N5O4
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity105.244
HBA5
HBD1
Rotatable Bonds4
Heavy Atoms28
LogP1.765
Activity (Ki) in nM158.489
Polar Surface Area (PSA)91.15
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 binding0.55715876
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms5
Fraction csp30.74
Ilogp2.75
Xlogp30.92
Wlogp0.04
Mlogp0.33
Silicos-it log p0.72
Consensus log p0.95
Esol log s-2.53
Esol solubility (mg/ml)1.16E+00
Esol solubility (mol/l)2.96E-03
Esol classSoluble
Ali log s-2.42
Ali solubility (mg/ml)1.50E+00
Ali solubility (mol/l)3.80E-03
Ali classSoluble
Silicos-it logsw-2.98
Silicos-it solubility (mg/ml)4.15E-01
Silicos-it solubility (mol/l)1.05E-03
Silicos-it classSoluble
Pgp substrate
Log kp (cm/s)-8.05
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 accessibility3.93
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-1.287
Logd1.509
Logp1.485
F (20%)0.945
F (30%)0.816
Mdck6.92E-06
Ppb0.6507
Vdss0.984
Fu0.5066
Cyp1a2-inh0.017
Cyp1a2-sub0.111
Cyp2c19-inh0.33
Cyp2c19-sub0.833
Cl5.42
T120.659
H-ht0.932
Dili0.805
Roa0.853
Fdamdd0.044
Skinsen0.674
Ec0.003
Ei0.011
Respiratory0.284
Bcf0.187
Igc501.951
Lc502.194
Lc50dm3.343
Nr-ar0.554
Nr-ar-lbd0.012
Nr-ahr0.055
Nr-aromatase0.006
Nr-er0.34
Nr-er-lbd0.009
Nr-ppar-gamma0.006
Sr-are0.615
Sr-atad50.006
Sr-hse0.01
Sr-mmp0.023
Sr-p530.018
Vol391.11
Dense1.005
Flex21
Nstereo0.286
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization2
Acute aquatic toxicity0
Toxicophores0
Qed2
Synth0.802
Fsp33.158
Mce-180.737
Natural product-likeness48.364
Alarm nmr-1.322
Bms2
Chelating0
Pfizer0
GskAccepted
GoldentriangleAccepted