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Assay Detail

CHEMBL615759

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Binding
In vitro affinity at human cloned 5-hydroxytryptamine 1A receptor by [3H]8-OH-DPAT displacement.
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors.
Glennon RA, Hong SS, Bondarev M, Law H, Dukat M, Rakhi S, Power P, Fan E, Kinneau D, Kamboj R, Teitler M, Herrick-Davis K, Smith C.
J Med Chem (1996) 39 : 314 -322
PubMed 8568822 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 6.89 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110317 ACETRYPTINE 2.0 1 8.89
CHEMBL8165 5-METHOXYTRYPTAMINE 1 8.49
CHEMBL321190 1 8.03
CHEMBL50492 1 7.82
CHEMBL107511 1 7.70
CHEMBL320079 1 7.42
CHEMBL111376 1 7.38
CHEMBL326667 2 7.32
CHEMBL107617 1 7.20
CHEMBL109526 1 7.06
CHEMBL128 SUMATRIPTAN 4.0 1 6.48
CHEMBL322349 1 6.39
CHEMBL322054 1 6.24
CHEMBL111284 1 6.24
CHEMBL110318 1 6.10
CHEMBL109839 1 6.05
CHEMBL111150 1 6.04
CHEMBL111283 1 5.93
CHEMBL418823 1 5.81
CHEMBL414420 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110317 ACETRYPTINE Ki = 1.3 nM 8.89
CHEMBL8165 5-METHOXYTRYPTAMINE Ki = 3.2 nM 8.49
CHEMBL321190 Ki = 9.3 nM 8.03
CHEMBL50492 Ki = 15.0 nM 7.82
CHEMBL107511 Ki = 20.0 nM 7.70
CHEMBL320079 Ki = 38.0 nM 7.42
CHEMBL111376 Ki = 42.0 nM 7.38
CHEMBL326667 Ki = 48.0 nM 7.32
CHEMBL107617 Ki = 63.0 nM 7.20
CHEMBL109526 Ki = 88.0 nM 7.06
CHEMBL326667 Ki = 315.0 nM 6.50
CHEMBL128 SUMATRIPTAN Ki = 330.0 nM 6.48
CHEMBL322349 Ki = 405.0 nM 6.39
CHEMBL322054 Ki = 575.0 nM 6.24
CHEMBL111284 Ki = 575.0 nM 6.24
CHEMBL110318 Ki = 800.0 nM 6.10
CHEMBL109839 Ki = 885.0 nM 6.05
CHEMBL111150 Ki = 920.0 nM 6.04
CHEMBL111283 Ki = 1180.0 nM 5.93
CHEMBL418823 Ki = 1550.0 nM 5.81
CHEMBL414420 Ki = 2300.0 nM 5.64