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Assay Detail

CHEMBL746874

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

Binding
Binding affinity against N-methyl-D-aspartate glutamate receptor using [3H]25-6981 as radioligand.
29
Total Activities
28
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

4-Aminoquinolines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
Pinard E, Alanine A, Bourson A, Büttelmann B, Heitz M, Mutela Ramanjit Gill V, Trube G, Wyler R.
Bioorg Med Chem Lett (2002) 12 : 2615 -2619
PubMed 12182873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 6.80 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50872 1 8.46
CHEMBL430457 1 8.00
CHEMBL89765 1 8.00
CHEMBL89134 2 7.96
CHEMBL88330 1 7.82
CHEMBL327615 1 7.77
CHEMBL89173 1 7.72
CHEMBL327643 1 7.66
CHEMBL90216 1 7.64
CHEMBL90161 1 7.58
CHEMBL84677 1 7.12
CHEMBL89098 1 7.00
CHEMBL90046 1 6.96
CHEMBL421728 1 6.58
CHEMBL88556 1 6.58
CHEMBL50608 1 6.38
CHEMBL89068 1 6.35
CHEMBL329112 1 6.30
CHEMBL327412 1 5.72
CHEMBL446677 1 5.43
CHEMBL421166 1 5.31
CHEMBL85349 1 5.12
CHEMBL89617 1 5.10
CHEMBL313723 1 4.48
CHEMBL328364 1 -
CHEMBL89786 2-PHENYLQUINOLINE 1 -
CHEMBL86510 1 -
CHEMBL89353 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50872 Ki = 3.5 nM 8.46
CHEMBL430457 Ki = 10.0 nM 8.00
CHEMBL89765 Ki = 10.0 nM 8.00
CHEMBL89134 Ki = 11.0 nM 7.96
CHEMBL88330 Ki = 15.0 nM 7.82
CHEMBL327615 Ki = 17.0 nM 7.77
CHEMBL89173 Ki = 19.0 nM 7.72
CHEMBL327643 Ki = 22.0 nM 7.66
CHEMBL90216 Ki = 23.0 nM 7.64
CHEMBL90161 Ki = 26.0 nM 7.58
CHEMBL84677 Ki = 75.0 nM 7.12
CHEMBL89134 Ki = 100.0 nM 7.00
CHEMBL89098 Ki = 100.0 nM 7.00
CHEMBL90046 Ki = 110.0 nM 6.96
CHEMBL88556 Ki = 260.0 nM 6.58
CHEMBL421728 Ki = 260.0 nM 6.58
CHEMBL50608 Ki = 413.0 nM 6.38
CHEMBL89068 Ki = 450.0 nM 6.35
CHEMBL329112 Ki = 500.0 nM 6.30
CHEMBL327412 Ki = 1900.0 nM 5.72
CHEMBL446677 Ki = 3700.0 nM 5.43
CHEMBL421166 Ki = 4900.0 nM 5.31
CHEMBL85349 Ki = 7500.0 nM 5.12
CHEMBL89617 Ki = 7900.0 nM 5.10
CHEMBL313723 Ki = 33000.0 nM 4.48
CHEMBL89786 2-PHENYLQUINOLINE Ki > 35000.0 nM -
CHEMBL86510 Ki > 40000.0 nM -
CHEMBL328364 Ki > 35000.0 nM -
CHEMBL89353 Ki > 4000.0 nM -