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Assay Detail

CHEMBL5442180

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Binding
PDSP Secondary Binding target: HTR1D - 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 ↗
32
Total Activities
32
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 1D (CHEMBL1983) ↗
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 32 6.30 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164327 — — 1 8.26
CHEMBL5089005 — — 1 7.83
CHEMBL2105760 BREXPIPRAZOLE 4.0 1 7.62
CHEMBL1516474 TEGASEROD MALEATE 4.0 1 7.30
CHEMBL4743049 — — 1 7.16
CHEMBL2024517 CARIPRAZINE HYDROCHLORIDE 4.0 1 7.11
CHEMBL24778 SILODOSIN 4.0 1 7.04
CHEMBL1200492 NEFAZODONE HYDROCHLORIDE 4.0 1 6.92
CHEMBL5075931 — — 1 6.67
CHEMBL1766103 — — 1 6.54
CHEMBL281350 SB-224289 — 1 6.43
CHEMBL1615374 VILAZODONE HYDROCHLORIDE 4.0 1 6.43
CHEMBL589390 LATREPIRDINE 3.0 1 6.38
CHEMBL1215661 PRUVANSERIN 2.0 1 6.23
CHEMBL3039520 LASMIDITAN 4.0 1 6.06
CHEMBL1200809 AZELASTINE HYDROCHLORIDE 4.0 1 6.05
CHEMBL1263 SALMETEROL 4.0 1 5.99
CHEMBL542139 — — 1 5.97
CHEMBL543113 — — 1 5.95
CHEMBL4743495 — — 1 5.92
CHEMBL79834 SPIRAMIDE 2.0 1 5.89
CHEMBL21283 — — 1 5.82
CHEMBL1836317 — — 1 5.79
CHEMBL5076314 — — 1 5.79
CHEMBL1200776 CINACALCET HYDROCHLORIDE 4.0 1 5.77
CHEMBL1707 LOPERAMIDE HYDROCHLORIDE 4.0 1 5.58
CHEMBL531742 — — 1 5.56
CHEMBL214957 — — 1 5.45
CHEMBL23327 PURVALANOLA — 1 5.42
CHEMBL1256998 — — 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164327 — Ki = 5.504 nM 8.26
CHEMBL5089005 — Ki = 14.95 nM 7.83
CHEMBL2105760 BREXPIPRAZOLE Ki = 24.05 nM 7.62
CHEMBL1516474 TEGASEROD MALEATE Ki = 50.13 nM 7.30
CHEMBL4743049 — Ki = 69.45 nM 7.16
CHEMBL2024517 CARIPRAZINE HYDROCHLORIDE Ki = 76.84 nM 7.11
CHEMBL24778 SILODOSIN Ki = 91.69 nM 7.04
CHEMBL1200492 NEFAZODONE HYDROCHLORIDE Ki = 121.68 nM 6.92
CHEMBL5075931 — Ki = 216.42 nM 6.67
CHEMBL1766103 — Ki = 291.75 nM 6.54
CHEMBL281350 SB-224289 Ki = 367.88 nM 6.43
CHEMBL1615374 VILAZODONE HYDROCHLORIDE Ki = 368.59 nM 6.43
CHEMBL589390 LATREPIRDINE Ki = 418.5 nM 6.38
CHEMBL1215661 PRUVANSERIN Ki = 588.3 nM 6.23
CHEMBL3039520 LASMIDITAN Ki = 869.36 nM 6.06
CHEMBL1200809 AZELASTINE HYDROCHLORIDE Ki = 885.42 nM 6.05
CHEMBL1263 SALMETEROL Ki = 1036.33 nM 5.99
CHEMBL542139 — Ki = 1078.2 nM 5.97
CHEMBL543113 — Ki = 1128.89 nM 5.95
CHEMBL4743495 — Ki = 1193.58 nM 5.92
CHEMBL79834 SPIRAMIDE Ki = 1287.51 nM 5.89
CHEMBL21283 — Ki = 1531.09 nM 5.82
CHEMBL1836317 — Ki = 1608.98 nM 5.79
CHEMBL5076314 — Ki = 1620.5 nM 5.79
CHEMBL1200776 CINACALCET HYDROCHLORIDE Ki = 1695.7 nM 5.77
CHEMBL1707 LOPERAMIDE HYDROCHLORIDE Ki = 2603.16 nM 5.58
CHEMBL531742 — Ki = 2775.24 nM 5.56
CHEMBL214957 — Ki = 3562.46 nM 5.45
CHEMBL23327 PURVALANOLA Ki = 3798.83 nM 5.42
CHEMBL1256998 — Ki = 3782.25 nM 5.42
CHEMBL1235246 — Ki = 8515.3 nM 5.07
CHEMBL88147 — Ki > 10000.0 nM -