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Assay Detail

CHEMBL2065481

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Binding
Displacement of [125I]O-iodo-trans-decalinvesamicol from VAChT in Sprague-Dawley rat cerebral membrane after 1 hr by gamma counting
9
Total Activities
9
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

Vesicular acetylcholine transporter (CHEMBL2125)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).
Kozaka T, Uno I, Kitamura Y, Miwa D, Ogawa K, Shiba K.
Bioorg Med Chem (2012) 20 : 4936 -4941
PubMed 22831799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.87 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064616 1 8.03
CHEMBL2064615 1 7.54
CHEMBL20943 1 7.48
CHEMBL12980 QUINUCLIDINYL BENZILATE 1 6.24
CHEMBL267930 SPIPERONE 2.0 1 5.99
CHEMBL282433 DITOLYLGUANIDINE 1 5.95
CHEMBL60542 (+)-PENTAZOCINE 1 -
CHEMBL51 KETANSERIN 3.0 1 -
CHEMBL1437 NOREPINEPHRINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064616 Ki = 9.3 nM 8.03
CHEMBL2064615 Ki = 28.6 nM 7.54
CHEMBL20943 Ki = 32.9 nM 7.48
CHEMBL12980 QUINUCLIDINYL BENZILATE Ki = 581.7 nM 6.24
CHEMBL267930 SPIPERONE Ki = 1033.0 nM 5.99
CHEMBL282433 DITOLYLGUANIDINE Ki = 1134.0 nM 5.95
CHEMBL60542 (+)-PENTAZOCINE Ki > 10000.0 nM -
CHEMBL51 KETANSERIN Ki > 10000.0 nM -
CHEMBL1437 NOREPINEPHRINE Ki > 10000.0 nM -