General Information
ZINC ID ZINC000071319304
Molecular Weight (Da)442
SMILESCC(C)(C)c1cc(NC(=O)N2CCCN(C(=O)CN3CCS(=O)(=O)CC3)CC2)no1
Molecular FormulaC19N5O5S1
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity112.266
HBA6
HBD1
Rotatable Bonds4
Heavy Atoms30
LogP1.494
Activity (Ki) in nM107.152
Polar Surface Area (PSA)124.44
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 binding0.56391686
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms5
Fraction csp30.74
Ilogp2.21
Xlogp30.44
Wlogp0.52
Mlogp0.21
Silicos-it log p0.03
Consensus log p0.68
Esol log s-2.52
Esol solubility (mg/ml)1.35E+00
Esol solubility (mol/l)3.05E-03
Esol classSoluble
Ali log s-2.62
Ali solubility (mg/ml)1.06E+00
Ali solubility (mol/l)2.39E-03
Ali classSoluble
Silicos-it logsw-3.12
Silicos-it solubility (mg/ml)3.36E-01
Silicos-it solubility (mol/l)7.62E-04
Silicos-it classSoluble
Pgp substrate
Log kp (cm/s)-8.68
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 accessibility4.08
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-1.376
Logd0.897
Logp0.611
F (20%)0.733
F (30%)0.896
Mdck6.33E-06
Ppb0.5806
Vdss1.396
Fu0.5643
Cyp1a2-inh0.007
Cyp1a2-sub0.11
Cyp2c19-inh0.053
Cyp2c19-sub0.794
Cl4.702
T120.747
H-ht0.923
Dili0.847
Roa0.628
Fdamdd0.08
Skinsen0.174
Ec0.003
Ei0.013
Respiratory0.198
Bcf0.162
Igc501.989
Lc502.128
Lc50dm3.489
Nr-ar0.671
Nr-ar-lbd0.074
Nr-ahr0.018
Nr-aromatase0.003
Nr-er0.245
Nr-er-lbd0.554
Nr-ppar-gamma0.03
Sr-are0.698
Sr-atad50.014
Sr-hse0.009
Sr-mmp0.019
Sr-p530.071
Vol418.409
Dense1.054
Flex23
Nstereo0.261
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization1
Acute aquatic toxicity0
Toxicophores0
Qed2
Synth0.7
Fsp33.389
Mce-180.737
Natural product-likeness56
Alarm nmr-1.358
Bms3
Chelating0
Pfizer0
GskAccepted
GoldentriangleRejected