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Assay Detail

CHEMBL2379284

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

Binding
Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in rat hippocampal membranes after 20 mins
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of novel pyrrolidine-2,5-dione derivatives as potential antidepressant agents. Part 1.
Wróbel MZ, Chodkowski A, Herold F, Gomółka A, Kleps J, Mazurek AP, Pluciński F, Mazurek A, Nowak G, Siwek A, Stachowicz K, Sławińska A, Wolak M, Szewczyk B, Satała G, Bojarski AJ, Turło J.
Eur J Med Chem (2013) 63 : 484 -500
PubMed 23524160 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.20 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 8.68
CHEMBL2377591 1 8.66
CHEMBL2377578 1 8.49
CHEMBL2377590 1 8.12
CHEMBL2377445 1 8.09
CHEMBL2377574 1 7.90
CHEMBL2377589 1 7.80
CHEMBL2377577 1 7.75
CHEMBL2377443 1 7.49
CHEMBL2377576 1 7.23
CHEMBL2377575 1 7.16
CHEMBL2377592 1 7.16
CHEMBL2377582 1 6.97
CHEMBL2377581 1 6.96
CHEMBL2377442 1 6.92
CHEMBL2377579 1 6.79
CHEMBL2377583 1 6.68
CHEMBL2377584 1 6.60
CHEMBL2377580 1 6.54
CHEMBL2377586 1 6.49
CHEMBL2377446 1 6.45
CHEMBL2377444 1 6.44
CHEMBL2377587 1 6.43
CHEMBL2377585 1 6.39
CHEMBL2377588 1 5.76
CHEMBL41 FLUOXETINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN Ki = 2.1 nM 8.68
CHEMBL2377591 Ki = 2.2 nM 8.66
CHEMBL2377578 Ki = 3.2 nM 8.49
CHEMBL2377590 Ki = 7.5 nM 8.12
CHEMBL2377445 Ki = 8.1 nM 8.09
CHEMBL2377574 Ki = 12.5 nM 7.90
CHEMBL2377589 Ki = 15.7 nM 7.80
CHEMBL2377577 Ki = 17.6 nM 7.75
CHEMBL2377443 Ki = 32.6 nM 7.49
CHEMBL2377576 Ki = 59.1 nM 7.23
CHEMBL2377575 Ki = 68.7 nM 7.16
CHEMBL2377592 Ki = 68.5 nM 7.16
CHEMBL2377582 Ki = 106.3 nM 6.97
CHEMBL2377581 Ki = 110.8 nM 6.96
CHEMBL2377442 Ki = 121.6 nM 6.92
CHEMBL2377579 Ki = 161.4 nM 6.79
CHEMBL2377583 Ki = 210.0 nM 6.68
CHEMBL2377584 Ki = 249.5 nM 6.60
CHEMBL2377580 Ki = 285.2 nM 6.54
CHEMBL2377586 Ki = 323.8 nM 6.49
CHEMBL2377446 Ki = 351.7 nM 6.45
CHEMBL2377444 Ki = 364.4 nM 6.44
CHEMBL2377587 Ki = 371.7 nM 6.43
CHEMBL2377585 Ki = 406.0 nM 6.39
CHEMBL2377588 Ki = 1740.4 nM 5.76
CHEMBL41 FLUOXETINE Ki - -