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Assay Detail

CHEMBL5215990

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Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
12
Total Activities
12
Compounds Tested
1
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 6 (CHEMBL3371)
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 12 8.09 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1083390 INTEPIRDINE 3.0 1 9.60
CHEMBL3329435 PF-05212377 2.0 1 9.28
CHEMBL362628 1 9.24
CHEMBL1085113 1 9.20
CHEMBL3286580 IDALOPIRDINE 3.0 1 9.08
CHEMBL2103880 CERLAPIRDINE 2.0 1 8.89
CHEMBL4117763 1 8.70
CHEMBL392760 1 8.66
CHEMBL589390 LATREPIRDINE 3.0 1 7.47
CHEMBL1580288 1 6.92
CHEMBL5219333 1 5.02
CHEMBL5219968 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1083390 INTEPIRDINE Ki = 0.25 nM 9.60
CHEMBL3329435 PF-05212377 Ki = 0.53 nM 9.28
CHEMBL362628 Ki = 0.58 nM 9.24
CHEMBL1085113 Ki = 0.63 nM 9.20
CHEMBL3286580 IDALOPIRDINE Ki = 0.83 nM 9.08
CHEMBL2103880 CERLAPIRDINE Ki = 1.3 nM 8.89
CHEMBL4117763 Ki = 2.0 nM 8.70
CHEMBL392760 Ki = 2.2 nM 8.66
CHEMBL589390 LATREPIRDINE Ki = 34.0 nM 7.47
CHEMBL1580288 Ki = 119.0 nM 6.92
CHEMBL5219333 Ki = 9617.0 nM 5.02
CHEMBL5219968 Ki = 9967.0 nM 5.00