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Assay Detail

CHEMBL5442206

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Binding
PDSP Secondary Binding target: HTR6 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL ↗
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

EUbOPEN Chemogenomics Library - PDSP Secondary Binding
EUbOPEN
(2024)
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.29 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5075931 — — 1 8.85
CHEMBL1489369 — — 1 6.90
CHEMBL589390 LATREPIRDINE 3.0 1 6.84
CHEMBL1200517 DIHYDROERGOTAMINE MESYLATE 4.0 1 6.65
CHEMBL180465 — — 1 6.55
CHEMBL267777 RITANSERIN 2.0 1 6.54
CHEMBL2105760 BREXPIPRAZOLE 4.0 1 6.51
CHEMBL1256863 — — 1 6.49
CHEMBL543113 — — 1 6.43
CHEMBL5076314 — — 1 6.42
CHEMBL79834 SPIRAMIDE 2.0 1 6.39
CHEMBL1671 PROPRANOLOL HYDROCHLORIDE 4.0 1 6.27
CHEMBL1516474 TEGASEROD MALEATE 4.0 1 6.25
CHEMBL1257131 RAUWOLSCINE HYDROCHLORIDE — 1 6.23
CHEMBL1633 KETOTIFEN FUMARATE 4.0 1 6.08
CHEMBL405355 NIGULDIPINE 2.0 1 6.06
CHEMBL1615374 VILAZODONE HYDROCHLORIDE 4.0 1 6.02
CHEMBL1200492 NEFAZODONE HYDROCHLORIDE 4.0 1 5.95
CHEMBL2024517 CARIPRAZINE HYDROCHLORIDE 4.0 1 5.89
CHEMBL103769 — — 1 5.88
CHEMBL1200776 CINACALCET HYDROCHLORIDE 4.0 1 5.74
CHEMBL1200809 AZELASTINE HYDROCHLORIDE 4.0 1 5.68
CHEMBL23327 PURVALANOLA — 1 5.64
CHEMBL2107572 TECALCET HYDROCHLORIDE 2.0 1 5.63
CHEMBL83894 FANANSERIN 2.0 1 5.29
CHEMBL1095777 INDACATEROL 4.0 1 -
CHEMBL1334465 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5075931 — Ki = 1.424 nM 8.85
CHEMBL1489369 — Ki = 125.33 nM 6.90
CHEMBL589390 LATREPIRDINE Ki = 143.87 nM 6.84
CHEMBL1200517 DIHYDROERGOTAMINE MESYLATE Ki = 224.56 nM 6.65
CHEMBL180465 — Ki = 280.06 nM 6.55
CHEMBL267777 RITANSERIN Ki = 286.85 nM 6.54
CHEMBL2105760 BREXPIPRAZOLE Ki = 308.35 nM 6.51
CHEMBL1256863 — Ki = 324.94 nM 6.49
CHEMBL543113 — Ki = 373.63 nM 6.43
CHEMBL5076314 — Ki = 377.83 nM 6.42
CHEMBL79834 SPIRAMIDE Ki = 405.23 nM 6.39
CHEMBL1671 PROPRANOLOL HYDROCHLORIDE Ki = 542.0 nM 6.27
CHEMBL1516474 TEGASEROD MALEATE Ki = 565.85 nM 6.25
CHEMBL1257131 RAUWOLSCINE HYDROCHLORIDE Ki = 588.17 nM 6.23
CHEMBL1633 KETOTIFEN FUMARATE Ki = 824.71 nM 6.08
CHEMBL405355 NIGULDIPINE Ki = 878.01 nM 6.06
CHEMBL1615374 VILAZODONE HYDROCHLORIDE Ki = 960.06 nM 6.02
CHEMBL1200492 NEFAZODONE HYDROCHLORIDE Ki = 1114.68 nM 5.95
CHEMBL2024517 CARIPRAZINE HYDROCHLORIDE Ki = 1301.37 nM 5.89
CHEMBL103769 — Ki = 1332.91 nM 5.88
CHEMBL1200776 CINACALCET HYDROCHLORIDE Ki = 1822.85 nM 5.74
CHEMBL1200809 AZELASTINE HYDROCHLORIDE Ki = 2092.42 nM 5.68
CHEMBL23327 PURVALANOLA Ki = 2265.43 nM 5.64
CHEMBL2107572 TECALCET HYDROCHLORIDE Ki = 2316.06 nM 5.63
CHEMBL83894 FANANSERIN Ki = 5105.05 nM 5.29
CHEMBL1095777 INDACATEROL Ki > 10000.0 nM -
CHEMBL1334465 — Ki > 10000.0 nM -