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Assay Detail

CHEMBL5531338

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Binding
Displacement of [3H]ifenprodil from rat GluN2B assessed as inhibition constant measured after 120 mins by competitive binding assay
ChEMBL ↗
55
Total Activities
55
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

Design, Synthesis, and Biological Evaluation of <i>Pierardine</i> Derivatives as Novel Brain-Penetrant and <i>In Vivo</i> Potent NMDAR-GluN2B Antagonists for Ischemic Stroke Treatment.
Lin G, Xu Q, Li J, Chu Z, Ma X, Zhu Q, Zhao Y, Mo J, Ye W, Shao L, Fang T, He M, Yue S, Dai M.
J Med Chem (2024) 67 : 3358 -3384
PubMed 38413367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 55 7.81 8.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5569595 — — 1 8.95
CHEMBL5595448 — — 1 8.89
CHEMBL5574644 — — 1 8.87
CHEMBL5563730 — — 1 8.73
CHEMBL5557099 — — 1 8.59
CHEMBL5573361 — — 1 8.54
CHEMBL5569472 — — 1 8.42
CHEMBL5549990 — — 1 8.37
CHEMBL5593442 — — 1 8.21
CHEMBL5571707 — — 1 8.20
CHEMBL5567278 — — 1 8.10
CHEMBL5573877 — — 1 8.09
CHEMBL5556777 — — 1 8.09
CHEMBL5571265 — — 1 8.03
CHEMBL5555022 — — 1 7.95
CHEMBL5555368 — — 1 7.92
CHEMBL5575712 — — 1 7.91
CHEMBL5564826 — — 1 7.89
CHEMBL5592128 — — 1 7.89
CHEMBL5566763 — — 1 7.88
CHEMBL5569343 — — 1 7.87
CHEMBL5592745 — — 1 7.86
CHEMBL5542853 — — 1 7.82
CHEMBL5572945 — — 1 7.82
CHEMBL5574263 — — 1 7.78
CHEMBL305187 IFENPRODIL 2.0 1 7.78
CHEMBL5594649 — — 1 7.71
CHEMBL5583544 — — 1 7.68
CHEMBL5590504 — — 1 7.63
CHEMBL5572431 — — 1 7.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5569595 — Ki = 1.12 nM 8.95
CHEMBL5595448 — Ki = 1.28 nM 8.89
CHEMBL5574644 — Ki = 1.34 nM 8.87
CHEMBL5563730 — Ki = 1.85 nM 8.73
CHEMBL5557099 — Ki = 2.6 nM 8.59
CHEMBL5573361 — Ki = 2.89 nM 8.54
CHEMBL5569472 — Ki = 3.77 nM 8.42
CHEMBL5549990 — Ki = 4.23 nM 8.37
CHEMBL5593442 — Ki = 6.12 nM 8.21
CHEMBL5571707 — Ki = 6.26 nM 8.20
CHEMBL5567278 — Ki = 7.97 nM 8.10
CHEMBL5573877 — Ki = 8.22 nM 8.09
CHEMBL5556777 — Ki = 8.15 nM 8.09
CHEMBL5571265 — Ki = 9.39 nM 8.03
CHEMBL5555022 — Ki = 11.34 nM 7.95
CHEMBL5555368 — Ki = 12.12 nM 7.92
CHEMBL5575712 — Ki = 12.36 nM 7.91
CHEMBL5564826 — Ki = 12.74 nM 7.89
CHEMBL5592128 — Ki = 12.99 nM 7.89
CHEMBL5566763 — Ki = 13.22 nM 7.88
CHEMBL5569343 — Ki = 13.4 nM 7.87
CHEMBL5592745 — Ki = 13.87 nM 7.86
CHEMBL5542853 — Ki = 15.22 nM 7.82
CHEMBL5572945 — Ki = 15.14 nM 7.82
CHEMBL305187 IFENPRODIL Ki = 16.7 nM 7.78
CHEMBL5574263 — Ki = 16.72 nM 7.78
CHEMBL5594649 — Ki = 19.61 nM 7.71
CHEMBL5583544 — Ki = 20.82 nM 7.68
CHEMBL5590504 — Ki = 23.64 nM 7.63
CHEMBL5572431 — Ki = 23.45 nM 7.63
CHEMBL5566951 — Ki = 24.27 nM 7.62
CHEMBL5590884 — Ki = 25.41 nM 7.59
CHEMBL5594184 — Ki = 25.92 nM 7.59
CHEMBL5574211 — Ki = 25.65 nM 7.59
CHEMBL5569695 — Ki = 26.03 nM 7.58
CHEMBL5594251 — Ki = 26.49 nM 7.58
CHEMBL5570408 — Ki = 26.8 nM 7.57
CHEMBL5594337 — Ki = 27.9 nM 7.55
CHEMBL5565776 — Ki = 29.16 nM 7.54
CHEMBL5568846 — Ki = 30.85 nM 7.51
CHEMBL5568694 — Ki = 31.12 nM 7.51
CHEMBL5570005 — Ki = 32.76 nM 7.49
CHEMBL5592653 — Ki = 32.11 nM 7.49
CHEMBL5563813 — Ki = 32.81 nM 7.48
CHEMBL5569784 — Ki = 33.61 nM 7.47
CHEMBL5571471 — Ki = 34.57 nM 7.46
CHEMBL5573394 — Ki = 36.22 nM 7.44
CHEMBL5563441 — Ki = 36.77 nM 7.43
CHEMBL5563987 — Ki = 42.93 nM 7.37
CHEMBL5557680 — Ki = 45.06 nM 7.35