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Assay Detail

CHEMBL3820054

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

Binding
Displacement of [3H]Ketanserin from human recombinant 5HT2A receptor incubated for 1.5 hrs by microbeta scintillation counting method
25
Total Activities
16
Compounds Tested
2
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 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.
Etukala JR, Zhu XY, Eyunni SV, Onyameh EK, Ofori E, Bricker BA, Kang HJ, Huang XP, Roth BL, Ablordeppey SY.
Bioorg Med Chem (2016) 24 : 3671 -3679
PubMed 27364609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 5.85 6.78
Inhibition 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3819642 2 6.78
CHEMBL3818799 2 6.29
CHEMBL3818478 2 6.01
CHEMBL3819403 2 5.97
CHEMBL3818124 2 5.95
CHEMBL2037520 2 5.81
CHEMBL3819153 2 5.47
CHEMBL2037526 2 5.43
CHEMBL2037432 2 5.37
CHEMBL3818940 1 5.22
CHEMBL3819567 1 -
CHEMBL3818935 1 -
CHEMBL3818398 1 -
CHEMBL3818805 1 -
CHEMBL3819434 1 -
CHEMBL3818881 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3819642 Ki = 165.96 nM 6.78
CHEMBL3819642 Ki = 168.0 nM 6.78
CHEMBL3818799 Ki = 519.0 nM 6.29
CHEMBL3818799 Ki = 524.81 nM 6.28
CHEMBL3818478 Ki = 977.24 nM 6.01
CHEMBL3818478 Ki = 982.0 nM 6.01
CHEMBL3819403 Ki = 1071.52 nM 5.97
CHEMBL3819403 Ki = 1082.0 nM 5.97
CHEMBL3818124 Ki = 1123.0 nM 5.95
CHEMBL2037520 Ki = 1564.0 nM 5.81
CHEMBL2037520 Ki = 1548.82 nM 5.81
CHEMBL3818124 Ki = 1584.89 nM 5.80
CHEMBL3819153 Ki = 3392.0 nM 5.47
CHEMBL3819153 Ki = 3388.44 nM 5.47
CHEMBL2037526 Ki = 3720.0 nM 5.43
CHEMBL2037526 Ki = 3715.35 nM 5.43
CHEMBL2037432 Ki = 4265.8 nM 5.37
CHEMBL2037432 Ki = 4255.0 nM 5.37
CHEMBL3818940 Ki = 5970.0 nM 5.22
CHEMBL3818881 Inhibition < 50.0 % -
CHEMBL3819434 Ki > 10000.0 nM -
CHEMBL3818805 Inhibition < 50.0 % -
CHEMBL3818398 Ki > 10000.0 nM -
CHEMBL3818935 Inhibition < 50.0 % -
CHEMBL3819567 Ki > 10000.0 nM -