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Assay Detail

CHEMBL895147

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

Binding
Displacement of [3H]CGP-39653 from rat NMDA receptor expressed in BHK cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.
Pellicciari R, Marinozzi M, Macchiarulo A, Fulco MC, Gafarova J, Serpi M, Giorgi G, Nielsen S, Thomsen C.
J Med Chem (2007) 50 : 4630 -4641
PubMed 17725337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.65 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282842 1 8.05
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.70
CHEMBL230951 1 5.57
CHEMBL389558 1 4.72
CHEMBL389556 1 4.66
CHEMBL230950 1 4.21
CHEMBL231157 1 -
CHEMBL389557 1 -
CHEMBL230949 1 -
CHEMBL389555 1 -
CHEMBL230852 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282842 Ki = 9.0 nM 8.05
CHEMBL575060 GLUTAMIC ACID Ki = 200.0 nM 6.70
CHEMBL230951 Ki = 2700.0 nM 5.57
CHEMBL389558 Ki = 19000.0 nM 4.72
CHEMBL389556 Ki = 22000.0 nM 4.66
CHEMBL230950 Ki = 61000.0 nM 4.21
CHEMBL231157 Ki > 300000.0 nM -
CHEMBL389557 Ki > 300000.0 nM -
CHEMBL230949 Ki > 300000.0 nM -
CHEMBL389555 Ki > 300000.0 nM -
CHEMBL230852 Ki = 150000.0 nM -