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Assay Detail

CHEMBL866803

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 porcine cortical membrane
26
Total Activities
26
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.
Enguehard-Gueiffier C, Hübner H, El Hakmaoui A, Allouchi H, Gmeiner P, Argiolas A, Melis MR, Gueiffier A.
J Med Chem (2006) 49 : 3938 -3947
PubMed 16789750 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.10 7.62
Ka 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378515 1 7.62
CHEMBL209034 1 6.44
CHEMBL211135 1 6.41
CHEMBL7927 FAUC 113 1 5.85
CHEMBL212370 1 5.77
CHEMBL212631 1 5.66
CHEMBL378680 1 5.64
CHEMBL380054 1 5.44
CHEMBL140099 1 -
CHEMBL42 CLOZAPINE 4.0 1 -
CHEMBL208274 1 -
CHEMBL212160 1 -
CHEMBL210551 1 -
CHEMBL211118 1 -
CHEMBL210283 1 -
CHEMBL210341 1 -
CHEMBL211539 1 -
CHEMBL379125 1 -
CHEMBL211590 1 -
CHEMBL143761 1 -
CHEMBL380287 1 -
CHEMBL207543 1 -
CHEMBL425064 1 -
CHEMBL377542 1 -
CHEMBL207488 1 -
CHEMBL211164 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378515 Ki = 24.0 nM 7.62
CHEMBL209034 Ki = 360.0 nM 6.44
CHEMBL211135 Ki = 390.0 nM 6.41
CHEMBL7927 FAUC 113 Ki = 1400.0 nM 5.85
CHEMBL212370 Ki = 1700.0 nM 5.77
CHEMBL212631 Ki = 2200.0 nM 5.66
CHEMBL378680 Ki = 2300.0 nM 5.64
CHEMBL380054 Ki = 3600.0 nM 5.44
CHEMBL140099 Ki - -
CHEMBL42 CLOZAPINE Ki - -
CHEMBL208274 Ki - -
CHEMBL212160 Ki - -
CHEMBL210551 Ki - -
CHEMBL211118 Ki - -
CHEMBL210283 Ki - -
CHEMBL210341 Ki - -
CHEMBL211539 Ki - -
CHEMBL379125 Ki - -
CHEMBL211590 Ki - -
CHEMBL143761 Ki - -
CHEMBL380287 Ki - -
CHEMBL207543 Ki - -
CHEMBL425064 Ki - -
CHEMBL377542 Ki - -
CHEMBL207488 Ki - -
CHEMBL211164 Ka - -