PF-06372865
Modify Date: 2025-08-21 05:51:19
PF-06372865 structure
|
Common Name | PF-06372865 | ||
|---|---|---|---|---|
| CAS Number | 1614245-70-3 | Molecular Weight | 440.493 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C22H21FN4O3S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of PF-06372865PF-06372865 is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator; exhibits functional selectivity for receptors containing α2/3/5 subunits, with significant positive allosteric modulation (90-140%) but negligible activity (<20%) at GABAA receptors containing α1 subunits; demonstrates a robust increase in saccadic peak velocity, increases in beta frequency qEEG and a slight saturating increase in body sway in clinical trials. Epilepsy Phase 1 Clinical |
| Name | PF-06372865 |
|---|
| Description | PF-06372865 is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator; exhibits functional selectivity for receptors containing α2/3/5 subunits, with significant positive allosteric modulation (90-140%) but negligible activity (<20%) at GABAA receptors containing α1 subunits; demonstrates a robust increase in saccadic peak velocity, increases in beta frequency qEEG and a slight saturating increase in body sway in clinical trials. Epilepsy Phase 1 Clinical |
|---|---|
| References | References 1. Nickolls SA, et al. Br J Pharmacol. 2018 Feb;175(4):708-725. View Related Products by Target GABA Receptor Epilepsy |
| Molecular Formula | C22H21FN4O3S |
|---|---|
| Molecular Weight | 440.493 |
| InChIKey | PTTQXDBPTFOCMT-UHFFFAOYSA-N |
| SMILES | CCn1cnc2c(-c3ccc(F)c(-c4ccc(S(=O)(=O)CC)cc4OC)c3)cnnc21 |
|
Name: Intrinsic clearance in rat hepatocytes assessed per million cells
Source: ChEMBL
Target: N/A
External Id: CHEMBL4351530
|
|
Name: Intrinsic clearance in human hepatocytes assessed per million cells
Source: ChEMBL
Target: N/A
External Id: CHEMBL4351529
|
|
Name: Intrinsic clearance in dog liver microsomes
Source: ChEMBL
Target: N/A
External Id: CHEMBL4351528
|
|
Name: Intrinsic clearance in rat liver microsomes
Source: ChEMBL
Target: N/A
External Id: CHEMBL4351527
|
|
Name: Substrate activity at BCRP (unknown origin) assessed as efflux ratio
Source: ChEMBL
Target: Broad substrate specificity ATP-binding cassette transporter ABCG2
External Id: CHEMBL4351526
|
|
Name: Substrate activity at P-gp (unknown origin) assessed as efflux ratio
Source: ChEMBL
Target: ATP-dependent translocase ABCB1
External Id: CHEMBL4351525
|
|
Name: Ratio of drug level in dog blood to plasma
Source: ChEMBL
Target: N/A
External Id: CHEMBL4351537
|
|
Name: Ratio of drug level in rat blood to plasma
Source: ChEMBL
Target: N/A
External Id: CHEMBL4351536
|
|
Name: Ratio of drug level in human blood to plasma
Source: ChEMBL
Target: N/A
External Id: CHEMBL4351535
|
Total 86, Current Page 1 of 9
1
2
3
4
5