TDI-11861 |
TDI-11861 : Inhibitor of ADCY10
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download
Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| ADCY10 |
|
|
Inhibitor
up to 100 nM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
TDI-11861 retained high selectivity for sAC vs closely related tmAC family members. TDI-11861 did no ...
Potency Cellular
In Vitro
ADCY10
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.2c01133
In Vivo Validations
Mouse
Dose: 2 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
0.93 ± 0.33 h
Systemic clearance:
94 ± 12 mL/min/Kg
Cmax:
2.5 ± 0.21 mM
Area Under the Curve::
0.78 ± 0.11 mM-h
DOI Reference: 10.1021/acs.jmedchem.2c01133
Dose: 10 mg/Kg
Route of delivery:
Oral
Cmax:
0.45 ± 0.015 mM
Tmax:
0.25 h
Area Under the Curve::
0.41 ± 0.057 mM-h
Bioavailability:
11 ± 1.4 %
DOI Reference: 10.1021/acs.jmedchem.2c01133
Dose: 50 mg/Kg
Route of delivery:
Oral
Cmax:
6.1 ± 1.9 mM
Tmax:
0.25 h
Area Under the Curve::
5.46 ± 1.5 mM-h
DOI Reference: 10.1021/acs.jmedchem.2c01133
Chemical Information
| Molecular Formula | C22H25ClF2N6O3 |
| InChI | InChI=1S/C22H25ClF2N6O3/c23-19-10-17(27-22(26)28-19)20-15(11-31(29-20)21(24)25)9-14-3-1-2-4-18(14)34-8-6-30-5-7-33-13-16(30)12-32/h1-4,10-11,16,21,32H,5-9,12-13H2,(H2,26,27,28)/t16-/m1/s1 |
| Molecular weight | 494.16 Da |
| AlogP | 0.0 |
| HBond acceptors | 9 |
| HBond donors | 3 |
| Atoms | 59 |