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Assay Detail

CHEMBL4339656

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

Binding
Displacement of [3H]-1-(azetidin-1-yl)-2-(6-(4-fluoro-3-methylphenyl)-1H-pyrrolo[3,2-b]pyridin-1-yl)ethanone from rat adult cortex GluN2B receptor measured after 2 hrs by liquid scintillation counting analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 2B (CHEMBL311)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.
Chrovian CC, Soyode-Johnson A, Wall JL, Rech JC, Schoellerman J, Lord B, Coe KJ, Carruthers NI, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA.
ACS Med Chem Lett (2019) 10 : 261 -266
PubMed 30891123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.55 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4443868 1 8.48
CHEMBL4529074 1 8.37
CHEMBL4547576 1 8.29
CHEMBL4550955 1 8.11
CHEMBL4445829 1 8.00
CHEMBL4302264 1 7.96
CHEMBL4474982 1 7.92
CHEMBL4571666 1 7.82
CHEMBL4515350 1 7.82
CHEMBL4531750 1 7.80
CHEMBL4593473 1 7.60
CHEMBL4211247 1 7.57
CHEMBL4588774 1 7.46
CHEMBL4575739 1 7.44
CHEMBL4451099 1 7.39
CHEMBL4451514 1 7.34
CHEMBL4529810 1 7.28
CHEMBL4591770 1 7.27
CHEMBL4539619 1 7.18
CHEMBL4446706 1 7.12
CHEMBL4471014 1 7.11
CHEMBL4467491 1 7.10
CHEMBL4590530 1 7.06
CHEMBL4475155 1 7.00
CHEMBL4464756 1 6.96
CHEMBL4526512 1 6.93
CHEMBL4537967 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4443868 Ki = 3.3 nM 8.48
CHEMBL4529074 Ki = 4.3 nM 8.37
CHEMBL4547576 Ki = 5.1 nM 8.29
CHEMBL4550955 Ki = 7.7 nM 8.11
CHEMBL4445829 Ki = 10.0 nM 8.00
CHEMBL4302264 Ki = 11.0 nM 7.96
CHEMBL4474982 Ki = 12.0 nM 7.92
CHEMBL4571666 Ki = 15.0 nM 7.82
CHEMBL4515350 Ki = 15.0 nM 7.82
CHEMBL4531750 Ki = 16.0 nM 7.80
CHEMBL4593473 Ki = 25.0 nM 7.60
CHEMBL4211247 Ki = 27.0 nM 7.57
CHEMBL4588774 Ki = 35.0 nM 7.46
CHEMBL4575739 Ki = 36.0 nM 7.44
CHEMBL4451099 Ki = 41.0 nM 7.39
CHEMBL4451514 Ki = 46.0 nM 7.34
CHEMBL4529810 Ki = 52.0 nM 7.28
CHEMBL4591770 Ki = 54.0 nM 7.27
CHEMBL4539619 Ki = 66.0 nM 7.18
CHEMBL4446706 Ki = 75.0 nM 7.12
CHEMBL4471014 Ki = 78.0 nM 7.11
CHEMBL4467491 Ki = 79.0 nM 7.10
CHEMBL4590530 Ki = 88.0 nM 7.06
CHEMBL4475155 Ki = 100.0 nM 7.00
CHEMBL4464756 Ki = 109.0 nM 6.96
CHEMBL4526512 Ki = 117.0 nM 6.93
CHEMBL4537967 Ki - -