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Assay Detail

CHEMBL5215977

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Binding
Binding affinity to 5-HT7R (unknown origin) assessed as inhibition constant
7
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chemical update on the potential for serotonin 5-HT<sub>6</sub> and 5-HT<sub>7</sub> receptor agents in the treatment of Alzheimer's disease.
Kucwaj-Brysz K, Baltrukevich H, Czarnota K, Handzlik J.
Bioorg Med Chem Lett (2021) 49 : 128275 -128275
PubMed 34311086 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.98 9.00
K 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5218527 1 9.00
CHEMBL4205783 JNJ-18038683 FREE BASE 2.0 1 8.52
CHEMBL589390 LATREPIRDINE 3.0 1 8.10
CHEMBL5219333 1 7.47
CHEMBL5219968 1 6.81
CHEMBL26 SULPIRIDE 3.0 1 -
CHEMBL5219924 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5218527 Ki = 1.0 nM 9.00
CHEMBL4205783 JNJ-18038683 FREE BASE Ki = 3.0 nM 8.52
CHEMBL589390 LATREPIRDINE Ki = 8.0 nM 8.10
CHEMBL5219333 Ki = 34.0 nM 7.47
CHEMBL5219968 Ki = 156.0 nM 6.81
CHEMBL26 SULPIRIDE Ki > 3000.0 nM -
CHEMBL5219924 K = 0.5 nM -