General Information
ZINC ID ZINC000218905198
Molecular Weight (Da)323
SMILESCC(C)n1nc(C(=O)NC(C)(C)c2ccccc2)c2c1[C@@H]1C[C@@H]1C2
Molecular FormulaC20N3O1
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity96.338
HBA2
HBD1
Rotatable Bonds4
Heavy Atoms24
LogP3.489
Activity (Ki) in nM18.621
Polar Surface Area (PSA)46.92
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 binding0.825
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms11
Fraction csp30.5
Ilogp2.91
Xlogp33.14
Wlogp3.68
Mlogp3.18
Silicos-it log p3.41
Consensus log p3.26
Esol log s-3.83
Esol solubility (mg/ml)0.0475
Esol solubility (mol/l)0.000147
Esol classSoluble
Ali log s-3.79
Ali solubility (mg/ml)0.0519
Ali solubility (mol/l)0.00016
Ali classSoluble
Silicos-it logsw-5.19
Silicos-it solubility (mg/ml)0.00208
Silicos-it solubility (mol/l)0.00000644
Silicos-it classModerately soluble
Pgp substrate
Log kp (cm/s)-6.04
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 violations0
Synthetic accessibility3.88
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-5.276
Logd3.983
Logp4.205
F (20%)0.002
F (30%)0.149
Mdck2.12E-05
Ppb0.9654
Vdss1.272
Fu0.031
Cyp1a2-inh0.424
Cyp1a2-sub0.245
Cyp2c19-inh0.853
Cyp2c19-sub0.92
Cl5.022
T120.145
H-ht0.476
Dili0.643
Roa0.081
Fdamdd0.793
Skinsen0.099
Ec0.003
Ei0.022
Respiratory0.945
Bcf0.93
Igc502.912
Lc504.339
Lc50dm4.069
Nr-ar0.002
Nr-ar-lbd0.002
Nr-ahr0.362
Nr-aromatase0.192
Nr-er0.296
Nr-er-lbd0.012
Nr-ppar-gamma0.011
Sr-are0.494
Sr-atad50.005
Sr-hse0.015
Sr-mmp0.427
Sr-p530.111
Vol346.212
Dense0.934
Flex0.278
Nstereo2
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization1
Acute aquatic toxicity0
Toxicophores0
Qed0.93
Synth3.464
Fsp30.5
Mce-1878.4
Natural product-likeness-0.86
Alarm nmr0
Bms0
Chelating0
Pfizer0
GskRejected
GoldentriangleAccepted