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TDI-10229 | TDI-10229 : Inhibitor of ADCY10
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ADCY10
  • IC50:195 nM
  • IC50:92 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
TDI-10229 did not show appreciable activity against a panel of 310 kinases and 46 other well-known d ...

Potency
Cellular
In Vitro

ADCY10

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acsmedchemlett.1c00273

In Vivo Validations

Mouse
Dose: 20 mg/kg
Route of delivery: Oral
Plasma half life: 3.95 h (MRT)
Cmax: 15.5 μM
Area Under the Curve:: 94 μM·h

DOI Reference: 10.1021/acsmedchemlett.1c00273

Dose: 20 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 2.82 h (MRT)
Cmax: 45 μM
Area Under the Curve:: 72 μM·h

DOI Reference: 10.1021/acsmedchemlett.1c00273

Negative Control Compounds

cpd 20
Notes: IC50 >10000 nM in biochemical assay

Chemical Information

Molecular Formula C16H16ClN5
SMILEs Cc1c(Cc2ccccc2)c(-c2cc(Cl)nc(N)n2)nn1C
InChI InChI=1S/C16H16ClN5/c1-10-12(8-11-6-4-3-5-7-11)15(21-22(10)2)13-9-14(17)20-16(18)19-13/h3-7,9H,8H2,1-2H3,(H2,18,19,20)
Molecular weight 313.11 Da
AlogP 3.011920000000001
HBond acceptors 5
HBond donors 2
Atoms 38

Vendors

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Expert Reviews

by SERP
(on 29 Aug 2023)
Cellular Use Rating
In Model Organisms
TDI-10229 appears to be a potent sAC inhibitor that is active both in vitro against purified enzyme and in cell assays of cAMP accumulation. Limited pharmacokinetic data provided for ip and po dosing in...
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