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Assay Detail

CHEMBL882176

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

Binding
In vitro inhibition of [3H]glycine at NMDA receptor
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
Leeson PD, Iversen LL.
J Med Chem (1994) 37 : 4053 -4067
PubMed 7990104 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 6.53 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32076 1 8.85
CHEMBL31741 1 8.70
CHEMBL39881 1 8.59
CHEMBL322420 1 8.16
CHEMBL287327 1 8.11
CHEMBL80741 1 8.10
CHEMBL114610 1 7.96
CHEMBL133163 1 7.72
CHEMBL131409 1 7.57
CHEMBL423518 1 7.51
CHEMBL22895 1 7.50
CHEMBL131520 1 7.50
CHEMBL265325 1-Aminocyclopropane carboxylic acid 1 7.40
CHEMBL105396 1 7.00
CHEMBL131842 1 7.00
CHEMBL300949 1 7.00
CHEMBL132501 1 6.96
CHEMBL96426 1 6.96
CHEMBL126035 1 6.92
CHEMBL293523 1 6.89
CHEMBL31344 1 6.85
CHEMBL113660 1 6.77
CHEMBL773 GLYCINE 4.0 1 6.70
CHEMBL50267 1 6.70
CHEMBL1744058 1 6.62
CHEMBL285123 (D)-SERINE 3.0 1 6.52
CHEMBL61315 1 6.44
CHEMBL131272 1 6.40
CHEMBL102574 1 6.39
CHEMBL334492 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32076 IC50 = 1.4 nM 8.85
CHEMBL31741 IC50 = 2.0 nM 8.70
CHEMBL39881 IC50 = 2.6 nM 8.59
CHEMBL322420 IC50 = 6.9 nM 8.16
CHEMBL287327 IC50 = 7.8 nM 8.11
CHEMBL80741 IC50 = 8.0 nM 8.10
CHEMBL114610 IC50 = 11.0 nM 7.96
CHEMBL133163 IC50 = 19.0 nM 7.72
CHEMBL131409 IC50 = 27.0 nM 7.57
CHEMBL423518 IC50 = 31.0 nM 7.51
CHEMBL22895 IC50 = 32.0 nM 7.50
CHEMBL131520 IC50 = 32.0 nM 7.50
CHEMBL265325 1-Aminocyclopropane carboxylic acid IC50 = 40.0 nM 7.40
CHEMBL131842 IC50 = 100.0 nM 7.00
CHEMBL105396 IC50 = 100.0 nM 7.00
CHEMBL300949 IC50 = 100.0 nM 7.00
CHEMBL132501 IC50 = 110.0 nM 6.96
CHEMBL96426 IC50 = 110.0 nM 6.96
CHEMBL126035 IC50 = 120.0 nM 6.92
CHEMBL293523 IC50 = 130.0 nM 6.89
CHEMBL31344 IC50 = 140.0 nM 6.85
CHEMBL113660 IC50 = 170.0 nM 6.77
CHEMBL773 GLYCINE IC50 = 200.0 nM 6.70
CHEMBL50267 IC50 = 200.0 nM 6.70
CHEMBL1744058 IC50 = 240.0 nM 6.62
CHEMBL285123 (D)-SERINE IC50 = 300.0 nM 6.52
CHEMBL61315 IC50 = 360.0 nM 6.44
CHEMBL131272 IC50 = 400.0 nM 6.40
CHEMBL102574 IC50 = 410.0 nM 6.39
CHEMBL334492 IC50 = 410.0 nM 6.39
CHEMBL115225 IC50 = 420.0 nM 6.38
CHEMBL130213 6,7-DICHLORO-3-HYDROXY-2-QUINOXALINECARBOXYLIC ACID IC50 = 460.0 nM 6.34
CHEMBL311389 7-CHLOROKYNURENIC ACID IC50 = 560.0 nM 6.25
CHEMBL277411 IC50 = 630.0 nM 6.20
CHEMBL553701 IC50 = 750.0 nM 6.12
CHEMBL130839 IC50 = 800.0 nM 6.10
CHEMBL23255 IC50 = 960.0 nM 6.02
CHEMBL323335 IC50 = 1000.0 nM 6.00
CHEMBL155265 DNQX IC50 = 1300.0 nM 5.89
CHEMBL131567 IC50 = 1300.0 nM 5.89
CHEMBL283819 IC50 = 1400.0 nM 5.85
CHEMBL771 CYCLOSERINE IC50 = 2300.0 nM 5.64
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE IC50 = 3100.0 nM 5.51
CHEMBL9790 IC50 = 4800.0 nM 5.32
CHEMBL325124 IC50 = 6000.0 nM 5.22
CHEMBL104297 IC50 = 6400.0 nM 5.19
CHEMBL335231 IC50 = 12500.0 nM 4.90
CHEMBL337030 IC50 = 19000.0 nM 4.72
CHEMBL131244 1-AMINOCYCLOBUTANE CARBOXYLIC ACID IC50 = 19000.0 nM 4.72
CHEMBL336423 IC50 = 36000.0 nM 4.44