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Assay Detail

CHEMBL615445

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

Binding
Ability to displace [3H]-DPAT from 5-hydroxytryptamine 1A receptor in homogenates of bovine hippocampus.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dopaminergic and serotonergic activities of imidazoquinolinones and related compounds.
Moon MW, Morris JK, Heier RF, Chidester CG, Hoffmann WE, Piercey MF, Althaus JS, Von Voigtlander PF, Evans DL, Figur LM.
J Med Chem (1992) 35 : 1076 -1092
PubMed 1348089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.04 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11577 1 8.62
CHEMBL273867 1 8.49
CHEMBL49 BUSPIRONE 4.0 1 8.18
CHEMBL1794795 1 7.92
CHEMBL1794997 1 7.90
CHEMBL269419 1 7.77
CHEMBL1202416 1 7.51
CHEMBL1202409 1 7.36
CHEMBL268274 1 7.31
CHEMBL1202412 1 7.08
CHEMBL12157 1 7.05
CHEMBL1744080 1 7.04
CHEMBL1202413 1 7.03
CHEMBL273711 1 7.02
CHEMBL1202407 1 6.99
CHEMBL1794998 1 6.98
CHEMBL11896 1 6.97
CHEMBL1202410 1 6.96
CHEMBL12021 1 6.77
CHEMBL267107 1 6.76
CHEMBL1794999 1 6.60
CHEMBL1202415 1 6.52
CHEMBL1202411 1 6.46
CHEMBL53 APOMORPHINE 4.0 1 6.27
CHEMBL274419 1 6.16
CHEMBL417612 1 6.08
CHEMBL275572 1 6.03
CHEMBL1202408 1 5.35
CHEMBL11729 1 -
CHEMBL1202414 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11577 Ki = 2.4 nM 8.62
CHEMBL273867 Ki = 3.2 nM 8.49
CHEMBL49 BUSPIRONE Ki = 6.6 nM 8.18
CHEMBL1794795 Ki = 12.0 nM 7.92
CHEMBL1794997 Ki = 12.5 nM 7.90
CHEMBL269419 Ki = 17.0 nM 7.77
CHEMBL1202416 Ki = 31.0 nM 7.51
CHEMBL1202409 Ki = 44.0 nM 7.36
CHEMBL268274 Ki = 49.0 nM 7.31
CHEMBL1202412 Ki = 84.0 nM 7.08
CHEMBL12157 Ki = 90.0 nM 7.05
CHEMBL1744080 Ki = 92.0 nM 7.04
CHEMBL1202413 Ki = 94.0 nM 7.03
CHEMBL273711 Ki = 95.0 nM 7.02
CHEMBL1202407 Ki = 102.0 nM 6.99
CHEMBL1794998 Ki = 105.0 nM 6.98
CHEMBL11896 Ki = 108.0 nM 6.97
CHEMBL1202410 Ki = 109.0 nM 6.96
CHEMBL12021 Ki = 171.0 nM 6.77
CHEMBL267107 Ki = 173.0 nM 6.76
CHEMBL1794999 Ki = 252.0 nM 6.60
CHEMBL1202415 Ki = 304.0 nM 6.52
CHEMBL1202411 Ki = 350.0 nM 6.46
CHEMBL53 APOMORPHINE Ki = 534.0 nM 6.27
CHEMBL274419 Ki = 687.0 nM 6.16
CHEMBL417612 Ki = 827.0 nM 6.08
CHEMBL275572 Ki = 933.0 nM 6.03
CHEMBL1202408 Ki = 4493.0 nM 5.35
CHEMBL11729 Ki > 1000.0 nM -
CHEMBL1202414 Ki > 1000.0 nM -
CHEMBL12285 Ki > 1000.0 nM -
CHEMBL441331 Ki > 1000.0 nM -