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Assay Detail

CHEMBL4670397

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 stably expressed in CHO-K1 cell membranes measured after 60 mins by Microbeta2 scintillation counting method
ChEMBL ↗
34
Total Activities
34
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

Discovery of Novel pERK1/2- or β-Arrestin-Preferring 5-HT Receptor-Biased Agonists: Diversified Therapeutic-like versus Side Effect Profile.
Sniecikowska J,Gluch-Lutwin M,Bucki A,Więckowska A,Siwek A,Jastrzebska-Wiesek M,Partyka A,Wilczyńska D,Pytka K,Latacz G,Przejczowska-Pomierny K,Wyska E,Wesołowska A,Pawłowski M,Newman-Tancredi A,Kolaczkowski M
J Med Chem (2020) 63 : 10946 -10971
PubMed 32883072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 9.89 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4746386 — — 1 10.89
CHEMBL4760271 — — 1 10.80
CHEMBL4739908 — — 1 10.78
CHEMBL4752833 — — 1 10.69
CHEMBL4759759 — — 1 10.60
CHEMBL4777581 — — 1 10.53
CHEMBL4751777 — — 1 10.51
CHEMBL4790662 — — 1 10.50
CHEMBL4796345 — — 1 10.47
CHEMBL4757755 — — 1 10.35
CHEMBL4797282 — — 1 10.32
CHEMBL4752177 — — 1 10.27
CHEMBL4786067 — — 1 10.22
CHEMBL4756041 — — 1 10.22
CHEMBL4750444 — — 1 10.22
CHEMBL4741857 — — 1 10.21
CHEMBL4747425 — — 1 10.10
CHEMBL4755058 — — 1 10.08
CHEMBL4781985 — — 1 9.93
CHEMBL4744067 — — 1 9.86
CHEMBL4760621 — — 1 9.85
CHEMBL4756322 — — 1 9.71
CHEMBL4740430 — — 1 9.56
CHEMBL4760666 — — 1 9.52
CHEMBL4800575 — — 1 9.42
CHEMBL4743868 — — 1 9.37
CHEMBL56 8-OH-DPAT — 1 9.09
CHEMBL4753394 — — 1 8.91
CHEMBL230963 — — 1 8.66
CHEMBL4797752 — — 1 8.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4746386 — Ki = 0.01288 nM 10.89
CHEMBL4760271 — Ki = 0.01585 nM 10.80
CHEMBL4739908 — Ki = 0.0166 nM 10.78
CHEMBL4752833 — Ki = 0.02042 nM 10.69
CHEMBL4759759 — Ki = 0.02512 nM 10.60
CHEMBL4777581 — Ki = 0.02951 nM 10.53
CHEMBL4751777 — Ki = 0.0309 nM 10.51
CHEMBL4790662 — Ki = 0.03162 nM 10.50
CHEMBL4796345 — Ki = 0.03388 nM 10.47
CHEMBL4757755 — Ki = 0.04467 nM 10.35
CHEMBL4797282 — Ki = 0.04786 nM 10.32
CHEMBL4752177 — Ki = 0.0537 nM 10.27
CHEMBL4786067 — Ki = 0.06026 nM 10.22
CHEMBL4756041 — Ki = 0.06026 nM 10.22
CHEMBL4750444 — Ki = 0.06026 nM 10.22
CHEMBL4741857 — Ki = 0.06166 nM 10.21
CHEMBL4747425 — Ki = 0.07943 nM 10.10
CHEMBL4755058 — Ki = 0.08318 nM 10.08
CHEMBL4781985 — Ki = 0.1175 nM 9.93
CHEMBL4744067 — Ki = 0.138 nM 9.86
CHEMBL4760621 — Ki = 0.1413 nM 9.85
CHEMBL4756322 — Ki = 0.195 nM 9.71
CHEMBL4740430 — Ki = 0.2754 nM 9.56
CHEMBL4760666 — Ki = 0.302 nM 9.52
CHEMBL4800575 — Ki = 0.3802 nM 9.42
CHEMBL4743868 — Ki = 0.4266 nM 9.37
CHEMBL56 8-OH-DPAT Ki = 0.8128 nM 9.09
CHEMBL4753394 — Ki = 1.23 nM 8.91
CHEMBL230963 — Ki = 2.188 nM 8.66
CHEMBL4797752 — Ki = 3.89 nM 8.41
CHEMBL49 BUSPIRONE Ki = 5.012 nM 8.30
CHEMBL4747083 — Ki = 6.607 nM 8.18
CHEMBL4790600 — Ki = 0.008511 nM -
CHEMBL4756233 — Ki = 0.0001585 nM -