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Assay Detail

CHEMBL909971

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

Binding
Displacement of [3H]KA from high affinity KA receptor in rat cortical membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
Colotta V, Catarzi D, Varano F, Lenzi O, Filacchioni G, Costagli C, Galli A, Ghelardini C, Galeotti N, Gratteri P, Sgrignani J, Deflorian F, Moro S.
J Med Chem (2006) 49 : 6015 -6026
PubMed 17004715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.91 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL387402 1 6.21
CHEMBL217826 1 5.39
CHEMBL217551 1 5.27
CHEMBL385648 1 5.21
CHEMBL310286 1 5.16
CHEMBL385438 1 5.09
CHEMBL386418 1 5.00
CHEMBL217519 1 4.89
CHEMBL438473 1 4.89
CHEMBL372797 1 4.34
CHEMBL384572 1 4.28
CHEMBL387049 1 4.09
CHEMBL216390 1 4.00
CHEMBL80594 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL387402 IC50 = 620.0 nM 6.21
CHEMBL217826 IC50 = 4100.0 nM 5.39
CHEMBL217551 IC50 = 5400.0 nM 5.27
CHEMBL385648 IC50 = 6200.0 nM 5.21
CHEMBL310286 IC50 = 7000.0 nM 5.16
CHEMBL385438 IC50 = 8200.0 nM 5.09
CHEMBL386418 IC50 = 10000.0 nM 5.00
CHEMBL217519 IC50 = 12900.0 nM 4.89
CHEMBL438473 IC50 = 13000.0 nM 4.89
CHEMBL372797 IC50 = 46000.0 nM 4.34
CHEMBL384572 IC50 = 52000.0 nM 4.28
CHEMBL387049 IC50 = 81000.0 nM 4.09
CHEMBL216390 IC50 = 100000.0 nM 4.00
CHEMBL80594 IC50 = 140000.0 nM -