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Assay Detail

CHEMBL616069

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

Binding
Binding affinity against rat hippocampal 5-hydroxytryptamine 1A (5-HT1A) receptor determined using [3H]8-OH-DPAT as radioligand
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors.
Höök BB, Cortizo L, Johansson AM, Westlind-Danielsson A, Mohell N, Hacksell U.
J Med Chem (1996) 39 : 4036 -4043
PubMed 8831769 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 7.78 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL87195 1 9.15
CHEMBL555098 1 9.05
CHEMBL538787 1 8.96
CHEMBL26998 1 8.89
CHEMBL41436 1 8.74
CHEMBL87348 1 8.74
CHEMBL131449 1 8.74
CHEMBL131547 1 8.42
CHEMBL544838 1 8.31
CHEMBL441088 1 8.26
CHEMBL41716 1 8.21
CHEMBL338581 1 8.16
CHEMBL545069 1 8.16
CHEMBL545533 1 8.12
CHEMBL130922 1 8.08
CHEMBL337049 1 8.03
CHEMBL131501 1 8.02
CHEMBL542475 1 7.87
CHEMBL130524 1 7.87
CHEMBL540064 1 7.86
CHEMBL49 BUSPIRONE 4.0 1 7.82
CHEMBL88157 1 7.77
CHEMBL541333 1 7.74
CHEMBL131776 1 7.73
CHEMBL543660 1 7.73
CHEMBL22778 1 7.61
CHEMBL545298 1 7.52
CHEMBL130206 1 7.52
CHEMBL128187 1 7.49
CHEMBL542952 1 7.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL87195 Ki = 0.7 nM 9.15
CHEMBL555098 Ki = 0.9 nM 9.05
CHEMBL538787 Ki = 1.1 nM 8.96
CHEMBL26998 Ki = 1.3 nM 8.89
CHEMBL41436 Ki = 1.8 nM 8.74
CHEMBL87348 Ki = 1.8 nM 8.74
CHEMBL131449 Ki = 1.8 nM 8.74
CHEMBL131547 Ki = 3.8 nM 8.42
CHEMBL544838 Ki = 4.9 nM 8.31
CHEMBL441088 Ki = 5.5 nM 8.26
CHEMBL41716 Ki = 6.1 nM 8.21
CHEMBL545069 Ki = 6.9 nM 8.16
CHEMBL338581 Ki = 6.9 nM 8.16
CHEMBL545533 Ki = 7.5 nM 8.12
CHEMBL130922 Ki = 8.4 nM 8.08
CHEMBL337049 Ki = 9.3 nM 8.03
CHEMBL131501 Ki = 9.5 nM 8.02
CHEMBL542475 Ki = 13.6 nM 7.87
CHEMBL130524 Ki = 13.6 nM 7.87
CHEMBL540064 Ki = 13.9 nM 7.86
CHEMBL49 BUSPIRONE Ki = 15.0 nM 7.82
CHEMBL88157 Ki = 17.0 nM 7.77
CHEMBL541333 Ki = 18.2 nM 7.74
CHEMBL543660 Ki = 18.5 nM 7.73
CHEMBL131776 Ki = 18.5 nM 7.73
CHEMBL22778 Ki = 24.8 nM 7.61
CHEMBL545298 Ki = 30.1 nM 7.52
CHEMBL130206 Ki = 30.1 nM 7.52
CHEMBL128187 Ki = 32.7 nM 7.49
CHEMBL542952 Ki = 32.7 nM 7.49
CHEMBL542727 Ki = 35.0 nM 7.46
CHEMBL335095 Ki = 35.0 nM 7.46
CHEMBL88504 Ki = 56.0 nM 7.25
CHEMBL541859 Ki = 88.9 nM 7.05
CHEMBL130552 Ki = 88.9 nM 7.05
CHEMBL69985 Ki = 136.0 nM 6.87
CHEMBL541858 Ki = 136.0 nM 6.87
CHEMBL552643 Ki = 177.0 nM 6.75
CHEMBL130550 Ki = 250.0 nM 6.60
CHEMBL544362 Ki = 250.0 nM 6.60
CHEMBL339845 Ki = 490.0 nM 6.31
CHEMBL554241 Ki = 490.0 nM 6.31
CHEMBL542474 Ki < 0.3 nM -
CHEMBL555356 Ki < 0.3 nM -
CHEMBL558994 Ki < 0.3 nM -