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Assay Detail

CHEMBL956719

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

Binding
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat hippocampal membrane
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Hippocampus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The influence of an ethylene spacer on the 5-HT(1A) and 5-HT(2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones.
Zajdel P, Subra G, Verdie P, Bojarski AJ, Duszyńska B, Basista K, Obniska J, Martinez J, Pawłowski M.
Eur J Med Chem (2009) 44 : 800 -808
PubMed 18603331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 40 6.62 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377153 1 8.52
CHEMBL208905 1 8.40
CHEMBL514077 1 8.37
CHEMBL60322 1 8.24
CHEMBL209007 1 8.05
CHEMBL207087 1 7.77
CHEMBL378298 1 7.72
CHEMBL208735 1 7.72
CHEMBL514202 1 7.62
CHEMBL408589 1 7.58
CHEMBL49 BUSPIRONE 4.0 1 7.44
CHEMBL209060 1 7.40
CHEMBL515933 1 7.39
CHEMBL210107 1 7.20
CHEMBL210157 1 7.16
CHEMBL477871 1 7.11
CHEMBL478068 1 6.96
CHEMBL212039 1 6.64
CHEMBL477945 1 6.64
CHEMBL477027 1 6.46
CHEMBL477034 1 6.44
CHEMBL478251 1 6.41
CHEMBL208785 1 6.32
CHEMBL478269 1 6.30
CHEMBL476169 1 6.24
CHEMBL476010 1 6.24
CHEMBL476217 1 6.00
CHEMBL477414 1 5.82
CHEMBL476221 1 5.76
CHEMBL477427 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377153 Ki = 3.0 nM 8.52
CHEMBL208905 Ki = 4.0 nM 8.40
CHEMBL514077 Ki = 4.3 nM 8.37
CHEMBL60322 Ki = 5.7 nM 8.24
CHEMBL209007 Ki = 9.0 nM 8.05
CHEMBL207087 Ki = 17.0 nM 7.77
CHEMBL378298 Ki = 19.0 nM 7.72
CHEMBL208735 Ki = 19.0 nM 7.72
CHEMBL514202 Ki = 24.0 nM 7.62
CHEMBL408589 Ki = 26.0 nM 7.58
CHEMBL49 BUSPIRONE Ki = 36.0 nM 7.44
CHEMBL209060 Ki = 40.0 nM 7.40
CHEMBL515933 Ki = 41.0 nM 7.39
CHEMBL210107 Ki = 63.0 nM 7.20
CHEMBL210157 Ki = 69.0 nM 7.16
CHEMBL477871 Ki = 78.0 nM 7.11
CHEMBL478068 Ki = 111.0 nM 6.96
CHEMBL212039 Ki = 230.0 nM 6.64
CHEMBL477945 Ki = 227.0 nM 6.64
CHEMBL477027 Ki = 350.0 nM 6.46
CHEMBL477034 Ki = 360.0 nM 6.44
CHEMBL478251 Ki = 390.0 nM 6.41
CHEMBL208785 Ki = 480.0 nM 6.32
CHEMBL478269 Ki = 497.0 nM 6.30
CHEMBL476169 Ki = 580.0 nM 6.24
CHEMBL476010 Ki = 579.0 nM 6.24
CHEMBL476217 Ki = 1001.0 nM 6.00
CHEMBL477414 Ki = 1507.0 nM 5.82
CHEMBL476221 Ki = 1730.0 nM 5.76
CHEMBL477427 Ki = 1950.0 nM 5.71
CHEMBL478265 Ki = 2013.0 nM 5.70
CHEMBL476053 Ki = 2087.0 nM 5.68
CHEMBL514070 Ki = 3553.0 nM 5.45
CHEMBL476054 Ki = 3675.0 nM 5.43
CHEMBL477266 Ki = 3775.0 nM 5.42
CHEMBL477428 Ki = 6600.0 nM 5.18
CHEMBL476062 Ki = 7440.0 nM 5.13
CHEMBL476261 Ki = 7586.0 nM 5.12
CHEMBL515930 Ki = 8518.0 nM 5.07
CHEMBL476260 Ki = 10020.0 nM 5.00