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Assay Detail

CHEMBL5336974

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

Binding
Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor (unknown origin) assessed as inhibition constant by radioligand binding assay
22
Total Activities
22
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 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT<sub>6</sub> Agents with a Beneficial Neuroprotective Profile against Alzheimer's Disease.
Pyka P, Haberek W, Więcek M, Szymanska E, Ali W, Cios A, Jastrzębska-Więsek M, Satała G, Podlewska S, Di Giacomo S, Di Sotto A, Garbo S, Karcz T, Lambona C, Marocco F, Latacz G, Sudoł-Tałaj S, Mordyl B, Głuch-Lutwin M, Siwek A, Czarnota-Łydka K, Gogola D, Olejarz-Maciej A, Wilczyńska-Zawal N, Honkisz-Orzechowska E, Starek M, Dąbrowska M, Kucwaj-Brysz K, Fioravanti R, Nasim MJ, Hittinger M, Partyka A, Wesołowska A, Battistelli C, Zwergel C, Handzlik J.
J Med Chem (2024) 67 : 1580 -1610
PubMed 38190615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 5.57 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49 BUSPIRONE 4.0 1 7.50
CHEMBL5395867 1 6.05
CHEMBL5397704 1 5.94
CHEMBL5406837 1 5.76
CHEMBL5433300 1 5.72
CHEMBL5410706 1 5.68
CHEMBL5419441 1 5.64
CHEMBL5423649 1 5.54
CHEMBL5405562 1 5.52
CHEMBL5436003 1 5.45
CHEMBL5420304 1 5.43
CHEMBL5407925 1 5.43
CHEMBL5434373 1 5.42
CHEMBL5433857 1 5.39
CHEMBL5405414 1 5.38
CHEMBL5400892 1 5.33
CHEMBL5402096 1 5.29
CHEMBL4462404 1 5.28
CHEMBL5416678 1 5.23
CHEMBL5406900 1 5.22
CHEMBL4580959 1 5.18
CHEMBL5397523 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49 BUSPIRONE Ki = 32.0 nM 7.50
CHEMBL5395867 Ki = 893.0 nM 6.05
CHEMBL5397704 Ki = 1149.0 nM 5.94
CHEMBL5406837 Ki = 1718.0 nM 5.76
CHEMBL5433300 Ki = 1904.0 nM 5.72
CHEMBL5410706 Ki = 2070.0 nM 5.68
CHEMBL5419441 Ki = 2306.0 nM 5.64
CHEMBL5423649 Ki = 2900.0 nM 5.54
CHEMBL5405562 Ki = 2999.0 nM 5.52
CHEMBL5436003 Ki = 3533.0 nM 5.45
CHEMBL5420304 Ki = 3702.0 nM 5.43
CHEMBL5407925 Ki = 3671.0 nM 5.43
CHEMBL5434373 Ki = 3812.0 nM 5.42
CHEMBL5433857 Ki = 4084.0 nM 5.39
CHEMBL5405414 Ki = 4145.0 nM 5.38
CHEMBL5400892 Ki = 4645.0 nM 5.33
CHEMBL5402096 Ki = 5110.0 nM 5.29
CHEMBL4462404 Ki = 5311.0 nM 5.28
CHEMBL5416678 Ki = 5948.0 nM 5.23
CHEMBL5406900 Ki = 6071.0 nM 5.22
CHEMBL4580959 Ki = 6647.0 nM 5.18
CHEMBL5397523 Ki = 7614.0 nM 5.12