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Assay Detail

CHEMBL4200092

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

Binding
Displacement of [3H]glycine from NMDA receptor in rat cortical and hippocampal membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Intermediate

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
Baqi Y, Pillaiyar T, Abdelrahman A, Kaufmann O, Alshaibani S, Rafehi M, Ghasimi S, Akkari R, Ritter K, Simon K, Spinrath A, Kostenis E, Zhao Q, Köse M, Namasivayam V, Müller CE.
J Med Chem (2018) 61 : 8136 -8154
PubMed 30048589 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.41 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31344 1 6.77
CHEMBL295718 1 5.70
CHEMBL53914 1 5.40
CHEMBL417544 1 4.60
CHEMBL278097 1 4.57
CHEMBL53744 1 -
CHEMBL50784 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31344 IC50 = 170.0 nM 6.77
CHEMBL295718 IC50 = 2000.0 nM 5.70
CHEMBL53914 IC50 = 4000.0 nM 5.40
CHEMBL417544 IC50 = 25000.0 nM 4.60
CHEMBL278097 IC50 = 27000.0 nM 4.57
CHEMBL53744 IC50 > 100000.0 nM -
CHEMBL50784 IC50 > 1000000.0 nM -