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Assay Detail

CHEMBL3404181

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

Binding
Displacement of [3H]-5-HT from human 5-HT1A receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT₁A and 5-HT₇ receptor ligands.
Modica MN, Intagliata S, Pittalà V, Salerno L, Siracusa MA, Cagnotto A, Salmona M, Romeo G.
Bioorg Med Chem Lett (2015) 25 : 1427 -1430
PubMed 25759032 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.58 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL350221 OXITRIPTAN 3.0 1 9.04
CHEMBL3401493 1 8.99
CHEMBL3401488 1 8.98
CHEMBL56 8-OH-DPAT 1 8.58
CHEMBL3401479 1 8.53
CHEMBL3401491 1 8.49
CHEMBL574827 1 8.28
CHEMBL3401486 1 8.20
CHEMBL3401482 1 8.13
CHEMBL3401473 1 7.82
CHEMBL3401489 1 7.79
CHEMBL3401492 1 7.58
CHEMBL3401484 1 7.54
CHEMBL3401478 1 7.44
CHEMBL3401470 1 7.43
CHEMBL3401469 1 7.40
CHEMBL3401481 1 7.36
CHEMBL3401487 1 7.29
CHEMBL3401477 1 7.27
CHEMBL3401480 1 7.12
CHEMBL3401483 1 6.94
CHEMBL3401476 1 6.94
CHEMBL3401475 1 6.83
CHEMBL3401490 1 6.68
CHEMBL3401485 1 6.57
CHEMBL3401474 1 6.44
CHEMBL282199 1 5.04
CHEMBL3401472 1 -
CHEMBL3401471 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL350221 OXITRIPTAN Ki = 0.91 nM 9.04
CHEMBL3401493 Ki = 1.03 nM 8.99
CHEMBL3401488 Ki = 1.04 nM 8.98
CHEMBL56 8-OH-DPAT Ki = 2.65 nM 8.58
CHEMBL3401479 Ki = 2.96 nM 8.53
CHEMBL3401491 Ki = 3.23 nM 8.49
CHEMBL574827 Ki = 5.3 nM 8.28
CHEMBL3401486 Ki = 6.28 nM 8.20
CHEMBL3401482 Ki = 7.33 nM 8.13
CHEMBL3401473 Ki = 15.2 nM 7.82
CHEMBL3401489 Ki = 16.1 nM 7.79
CHEMBL3401492 Ki = 26.4 nM 7.58
CHEMBL3401484 Ki = 28.9 nM 7.54
CHEMBL3401478 Ki = 36.6 nM 7.44
CHEMBL3401470 Ki = 37.4 nM 7.43
CHEMBL3401469 Ki = 39.6 nM 7.40
CHEMBL3401481 Ki = 43.5 nM 7.36
CHEMBL3401487 Ki = 51.5 nM 7.29
CHEMBL3401477 Ki = 53.9 nM 7.27
CHEMBL3401480 Ki = 75.3 nM 7.12
CHEMBL3401483 Ki = 116.0 nM 6.94
CHEMBL3401476 Ki = 114.0 nM 6.94
CHEMBL3401475 Ki = 148.0 nM 6.83
CHEMBL3401490 Ki = 211.0 nM 6.68
CHEMBL3401485 Ki = 268.0 nM 6.57
CHEMBL3401474 Ki = 363.0 nM 6.44
CHEMBL282199 Ki = 9024.0 nM 5.04
CHEMBL3401472 Ki - -
CHEMBL3401471 Ki - -