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Assay Detail

CHEMBL2352644

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

Binding
Displacement of [3H]MK-801 from NMDA receptor complex (unknown origin) after 40 mins
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate [NMDA] receptor (CHEMBL2094124)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Improving the inhibitory activity of arylidenaminoguanidine compounds at the N-methyl-D-aspartate receptor complex from a recursive computational-experimental structure-activity relationship study.
Ring JR, Zheng F, Haubner AJ, Littleton JM, Crooks PA.
Bioorg Med Chem (2013) 21 : 1764 -1774
PubMed 23465801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 4.54 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54151 1 5.44
CHEMBL2346953 1 5.22
CHEMBL2346945 1 5.15
CHEMBL2346946 1 5.11
CHEMBL105167 1 5.10
CHEMBL2346939 1 5.07
CHEMBL2346937 1 5.06
CHEMBL2346943 1 4.99
CHEMBL2346935 1 4.94
CHEMBL105099 1 4.77
CHEMBL2346944 1 4.74
CHEMBL2346955 1 4.64
CHEMBL2346952 1 4.60
CHEMBL2346936 1 4.58
CHEMBL2346938 1 4.57
CHEMBL105703 1 4.54
CHEMBL534939 1 4.49
CHEMBL2346814 1 4.48
CHEMBL2346950 1 4.42
CHEMBL53180 1 4.41
CHEMBL2346954 1 4.37
CHEMBL2346956 1 4.36
CHEMBL2346815 1 4.31
CHEMBL2346816 1 4.30
CHEMBL2346940 1 4.26
CHEMBL2346817 1 4.24
CHEMBL2346812 1 4.23
CHEMBL2346947 1 4.20
CHEMBL2346959 1 4.15
CHEMBL296174 1 4.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54151 IC50 = 3630.78 nM 5.44
CHEMBL2346953 IC50 = 6025.6 nM 5.22
CHEMBL2346945 IC50 = 7079.46 nM 5.15
CHEMBL2346946 IC50 = 7762.47 nM 5.11
CHEMBL105167 IC50 = 7943.28 nM 5.10
CHEMBL2346939 IC50 = 8511.38 nM 5.07
CHEMBL2346937 IC50 = 8709.64 nM 5.06
CHEMBL2346943 IC50 = 10232.93 nM 4.99
CHEMBL2346935 IC50 = 11481.54 nM 4.94
CHEMBL105099 IC50 = 16982.44 nM 4.77
CHEMBL2346944 IC50 = 18197.01 nM 4.74
CHEMBL2346955 IC50 = 22908.68 nM 4.64
CHEMBL2346952 IC50 = 25118.86 nM 4.60
CHEMBL2346936 IC50 = 26302.68 nM 4.58
CHEMBL2346938 IC50 = 26915.35 nM 4.57
CHEMBL105703 IC50 = 28840.32 nM 4.54
CHEMBL534939 IC50 = 32359.37 nM 4.49
CHEMBL2346814 IC50 = 33113.11 nM 4.48
CHEMBL2346950 IC50 = 38018.94 nM 4.42
CHEMBL53180 IC50 = 38904.51 nM 4.41
CHEMBL2346954 IC50 = 42657.95 nM 4.37
CHEMBL2346956 IC50 = 43651.58 nM 4.36
CHEMBL2346815 IC50 = 48977.88 nM 4.31
CHEMBL2346816 IC50 = 50118.72 nM 4.30
CHEMBL2346940 IC50 = 54954.09 nM 4.26
CHEMBL2346817 IC50 = 57543.99 nM 4.24
CHEMBL2346812 IC50 = 58884.37 nM 4.23
CHEMBL2346947 IC50 = 63095.73 nM 4.20
CHEMBL2346959 IC50 = 70794.58 nM 4.15
CHEMBL296174 IC50 = 72443.6 nM 4.14
CHEMBL2346958 IC50 = 72443.6 nM 4.14
CHEMBL2346942 IC50 = 74131.02 nM 4.13
CHEMBL104315 IC50 = 77624.71 nM 4.11
CHEMBL320890 IC50 = 81283.05 nM 4.09
CHEMBL2346941 IC50 = 91201.08 nM 4.04
CHEMBL2346933 IC50 = 95499.26 nM 4.02
CHEMBL2346949 IC50 = 223872.11 nM -
CHEMBL2346951 IC50 = 213796.21 nM -
CHEMBL2346934 IC50 = 109647.82 nM -
CHEMBL2346948 IC50 = 109647.82 nM -
CHEMBL2346957 IC50 = 229086.77 nM -
CHEMBL2346932 IC50 = 676082.98 nM -
CHEMBL2346931 IC50 = 537031.8 nM -
CHEMBL2346813 IC50 = 181970.09 nM -
CHEMBL106177 IC50 = 154881.66 nM -