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Assay Detail

CHEMBL1059305

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

Binding
Displacement of [3H](+/-)-emopamil from EBP in Dunkin guinea pig liver membrane by radioreceptor binding assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Liver
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (CHEMBL5525)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Exploring the importance of piperazine N-atoms for sigma(2) receptor affinity and activity in a series of analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28).
Berardi F, Abate C, Ferorelli S, Uricchio V, Colabufo NA, Niso M, Perrone R.
J Med Chem (2009) 52 : 7817 -7828
PubMed 19842660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.49 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573932 1 8.84
CHEMBL574821 1 8.33
CHEMBL583580 1 8.13
CHEMBL573234 1 8.13
CHEMBL53325 1 8.08
CHEMBL305187 IFENPRODIL 2.0 1 7.99
CHEMBL573695 1 7.98
CHEMBL134607 1 7.96
CHEMBL573703 1 7.77
CHEMBL574598 1 7.64
CHEMBL582875 1 7.50
CHEMBL50079 1 7.45
CHEMBL584767 1 7.31
CHEMBL575238 1 7.19
CHEMBL573248 1 6.82
CHEMBL573704 1 6.64
CHEMBL575253 1 6.33
CHEMBL573461 1 6.26
CHEMBL575262 1 5.91
CHEMBL574182 1 -
CHEMBL574165 1 -
CHEMBL575239 1 -
CHEMBL576193 1 -
CHEMBL583945 1 -
CHEMBL574155 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573932 Ki = 1.46 nM 8.84
CHEMBL574821 Ki = 4.7 nM 8.33
CHEMBL583580 Ki = 7.4 nM 8.13
CHEMBL573234 Ki = 7.4 nM 8.13
CHEMBL53325 Ki = 8.38 nM 8.08
CHEMBL305187 IFENPRODIL Ki = 10.2 nM 7.99
CHEMBL573695 Ki = 10.4 nM 7.98
CHEMBL134607 Ki = 11.1 nM 7.96
CHEMBL573703 Ki = 17.0 nM 7.77
CHEMBL574598 Ki = 23.0 nM 7.64
CHEMBL582875 Ki = 32.0 nM 7.50
CHEMBL50079 Ki = 35.4 nM 7.45
CHEMBL584767 Ki = 49.0 nM 7.31
CHEMBL575238 Ki = 64.4 nM 7.19
CHEMBL573248 Ki = 150.0 nM 6.82
CHEMBL573704 Ki = 230.0 nM 6.64
CHEMBL575253 Ki = 470.0 nM 6.33
CHEMBL573461 Ki = 550.0 nM 6.26
CHEMBL575262 Ki = 1230.0 nM 5.91
CHEMBL574182 Ki > 1000.0 nM -
CHEMBL574165 Ki > 1000.0 nM -
CHEMBL575239 Ki > 1000.0 nM -
CHEMBL576193 Ki - -
CHEMBL583945 Ki - -
CHEMBL574155 Ki - -