General Information
ZINC ID ZINC000072105947
Molecular Weight (Da)438
SMILESCCCCCn1cc(C(=O)NC23CC4CC(CC(C4)C2)C3)c(=O)c2cccc([N+](=O)[O-])c21
Molecular FormulaC25N3O4
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity120.196
HBA2
HBD1
Rotatable Bonds7
Heavy Atoms32
LogP5.147
Activity (Ki) in nM1
Polar Surface Area (PSA)94.24
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
-
Biodegradation0
Glucocorticoid receptor binding+
Thyroid receptor binding+
Androgen receptor binding+
Plasma protein binding0.88517904
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms10
Fraction csp30.6
Ilogp2.98
Xlogp35.48
Wlogp4.8
Mlogp2.67
Silicos-it log p2.73
Consensus log p3.73
Esol log s-5.71
Esol solubility (mg/ml)0.000856
Esol solubility (mol/l)0.00000196
Esol classModerately
Ali log s-7.27
Ali solubility (mg/ml)0.0000233
Ali solubility (mol/l)5.33E-08
Ali classPoorly sol
Silicos-it logsw-6.12
Silicos-it solubility (mg/ml)0.00033
Silicos-it solubility (mol/l)0.00000075
Silicos-it classPoorly soluble
Pgp substrate
Log kp (cm/s)-5.08
Lipinski number of violations0
Ghose number of violations0
Veber number of violations0
Egan number of violations0
Muegge number of violations1
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts2
Leadlikeness number of violations3
Synthetic accessibility5.47
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-6.444
Logd4.352
Logp5.049
F (20%)0.001
F (30%)0.003
Mdck9.71E-05
Ppb0.9341
Vdss0.855
Fu0.0221
Cyp1a2-inh0.17
Cyp1a2-sub0.134
Cyp2c19-inh0.771
Cyp2c19-sub0.07
Cl1.796
T120.012
H-ht0.386
Dili0.301
Roa0.216
Fdamdd0.58
Skinsen0.138
Ec0.003
Ei0.021
Respiratory0.727
Bcf1.765
Igc504.934
Lc505.999
Lc50dm6.357
Nr-ar0.022
Nr-ar-lbd0.004
Nr-ahr0.577
Nr-aromatase0.138
Nr-er0.316
Nr-er-lbd0.023
Nr-ppar-gamma0.053
Sr-are0.649
Sr-atad50.009
Sr-hse0.861
Sr-mmp0.848
Sr-p530.715
Vol447.87
Dense0.976
Flex0.308
Nstereo0
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity5
Surechembl0
Nonbiodegradable3
Skin sensitization0
Acute aquatic toxicity0
Toxicophores4
Qed0.382
Synth3.809
Fsp30.6
Mce-1872.5
Natural product-likeness-0.976
Alarm nmr2
Bms0
Chelating0
Pfizer0
GskRejected
GoldentriangleAccepted