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Assay Detail

CHEMBL4815622

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

Binding
Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL ↗
42
Total Activities
23
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

New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.
Ofori E, Onyameh EK, Gonela UM, Voshavar C, Bricker B, Swanson TL, Eshleman AJ, Schmachtenberg JL, Bloom SH, Janowsky AJ, Ablordeppey SY.
Eur J Med Chem (2021) 214 : 113243 -113243
PubMed 33582388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 7.95 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4846823 — — 2 9.13
CHEMBL1940418 — — 1 8.96
CHEMBL4862180 — — 2 8.64
CHEMBL4871868 — — 2 8.62
CHEMBL4857665 — — 2 8.39
CHEMBL4857597 — — 2 8.39
CHEMBL4876297 — — 2 8.30
CHEMBL4874069 — — 2 8.28
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.25
CHEMBL4866058 — — 2 8.21
CHEMBL340211 AZAPERONE 2.0 2 8.12
CHEMBL4866053 — — 1 8.10
CHEMBL4871850 — — 1 7.94
CHEMBL4845741 — — 2 7.89
CHEMBL4859988 — — 2 7.85
CHEMBL4865591 — — 2 7.72
CHEMBL4870361 — — 2 7.72
CHEMBL4861794 — — 2 7.57
CHEMBL4872800 — — 2 7.50
CHEMBL4854456 — — 2 7.34
CHEMBL4845947 — — 2 7.33
CHEMBL4875079 — — 2 7.03
CHEMBL4859722 — — 2 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4846823 — Ki = 0.74 nM 9.13
CHEMBL4846823 — Ki = 0.7413 nM 9.13
CHEMBL1940418 — Ki = 1.1 nM 8.96
CHEMBL4862180 — Ki = 2.3 nM 8.64
CHEMBL4862180 — Ki = 2.344 nM 8.63
CHEMBL4871868 — Ki = 2.399 nM 8.62
CHEMBL4871868 — Ki = 2.45 nM 8.61
CHEMBL4857665 — Ki = 4.074 nM 8.39
CHEMBL4857597 — Ki = 4.074 nM 8.39
CHEMBL4857665 — Ki = 4.4 nM 8.36
CHEMBL4857597 — Ki = 4.5 nM 8.35
CHEMBL4876297 — Ki = 5.012 nM 8.30
CHEMBL4876297 — Ki = 5.1 nM 8.29
CHEMBL4874069 — Ki = 5.2 nM 8.28
CHEMBL4874069 — Ki = 5.248 nM 8.28
CHEMBL1112 ARIPIPRAZOLE Ki = 5.6 nM 8.25
CHEMBL4866058 — Ki = 6.166 nM 8.21
CHEMBL4866058 — Ki = 6.1 nM 8.21
CHEMBL340211 AZAPERONE Ki = 7.586 nM 8.12
CHEMBL4866053 — Ki = 8.0 nM 8.10
CHEMBL340211 AZAPERONE Ki = 8.1 nM 8.09
CHEMBL4871850 — Ki = 11.39 nM 7.94
CHEMBL4845741 — Ki = 13.0 nM 7.89
CHEMBL4845741 — Ki = 13.49 nM 7.87
CHEMBL4859988 — Ki = 14.0 nM 7.85
CHEMBL4859988 — Ki = 14.45 nM 7.84
CHEMBL4865591 — Ki = 19.05 nM 7.72
CHEMBL4870361 — Ki = 19.05 nM 7.72
CHEMBL4870361 — Ki = 19.0 nM 7.72
CHEMBL4865591 — Ki = 20.3 nM 7.69
CHEMBL4861794 — Ki = 27.0 nM 7.57
CHEMBL4861794 — Ki = 26.92 nM 7.57
CHEMBL4872800 — Ki = 32.0 nM 7.50
CHEMBL4872800 — Ki = 31.62 nM 7.50
CHEMBL4854456 — Ki = 46.0 nM 7.34
CHEMBL4845947 — Ki = 47.3 nM 7.33
CHEMBL4854456 — Ki = 46.77 nM 7.33
CHEMBL4845947 — Ki = 50.12 nM 7.30
CHEMBL4875079 — Ki = 93.0 nM 7.03
CHEMBL4875079 — Ki = 93.33 nM 7.03
CHEMBL4859722 — Ki = 411.0 nM 6.39
CHEMBL4859722 — Ki = 407.38 nM 6.39