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Assay Detail

CHEMBL876000

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
In vitro inhibitory concentration against glutamate stimulated accumulation of cyclic GMP in neonatal rat cerebral slices
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antagonist.
Baron BM, Cregge RJ, Farr RA, Friedrich D, Gross RS, Harrison BL, Janowick DA, Matthews D, McCloskey TC, Meikrantz S, Nyce PL, Vaz R, Metz WA.
J Med Chem (2005) 48 : 995 -1018
PubMed 15715469 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.69 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31741 1 7.51
CHEMBL289832 LICOSTINEL 2.0 1 6.74
CHEMBL419045 GAVESTINEL SODIUM 1 6.58
CHEMBL180427 1 6.55
CHEMBL425691 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31741 IC50 = 31.0 nM 7.51
CHEMBL289832 LICOSTINEL IC50 = 183.0 nM 6.74
CHEMBL419045 GAVESTINEL SODIUM IC50 = 262.0 nM 6.58
CHEMBL180427 IC50 = 282.0 nM 6.55
CHEMBL425691 IC50 = 840.0 nM 6.08