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Assay Detail

CHEMBL617320

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

Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
26
Total Activities
25
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 1B (CHEMBL1898)
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 26 7.90 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320079 1 9.00
CHEMBL326667 2 9.00
CHEMBL321190 1 8.96
CHEMBL111376 1 8.80
CHEMBL107617 1 8.70
CHEMBL111150 1 8.64
CHEMBL8165 5-METHOXYTRYPTAMINE 1 8.46
CHEMBL109526 1 8.34
CHEMBL50492 1 8.26
CHEMBL110317 ACETRYPTINE 2.0 1 8.13
CHEMBL107511 1 8.11
CHEMBL128 SUMATRIPTAN 4.0 1 8.00
CHEMBL111283 1 7.85
CHEMBL109839 1 7.68
CHEMBL110318 1 7.66
CHEMBL111284 1 7.46
CHEMBL6640 TRYPTAMINE 1 7.44
CHEMBL322054 1 7.40
CHEMBL107487 1 7.28
CHEMBL327103 1 7.28
CHEMBL322349 1 7.23
CHEMBL109360 1 7.20
CHEMBL418823 1 6.87
CHEMBL275854 1 6.60
CHEMBL414420 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL326667 Ki = 1.0 nM 9.00
CHEMBL320079 Ki = 1.0 nM 9.00
CHEMBL321190 Ki = 1.1 nM 8.96
CHEMBL111376 Ki = 1.6 nM 8.80
CHEMBL107617 Ki = 2.0 nM 8.70
CHEMBL111150 Ki = 2.3 nM 8.64
CHEMBL326667 Ki = 3.0 nM 8.52
CHEMBL8165 5-METHOXYTRYPTAMINE Ki = 3.5 nM 8.46
CHEMBL109526 Ki = 4.6 nM 8.34
CHEMBL50492 Ki = 5.5 nM 8.26
CHEMBL110317 ACETRYPTINE Ki = 7.4 nM 8.13
CHEMBL107511 Ki = 7.8 nM 8.11
CHEMBL128 SUMATRIPTAN Ki = 10.0 nM 8.00
CHEMBL111283 Ki = 14.0 nM 7.85
CHEMBL109839 Ki = 21.0 nM 7.68
CHEMBL110318 Ki = 22.0 nM 7.66
CHEMBL111284 Ki = 35.0 nM 7.46
CHEMBL6640 TRYPTAMINE Ki = 36.0 nM 7.44
CHEMBL322054 Ki = 40.0 nM 7.40
CHEMBL107487 Ki = 53.0 nM 7.28
CHEMBL327103 Ki = 52.0 nM 7.28
CHEMBL322349 Ki = 59.0 nM 7.23
CHEMBL109360 Ki = 63.0 nM 7.20
CHEMBL418823 Ki = 135.0 nM 6.87
CHEMBL275854 Ki = 250.0 nM 6.60
CHEMBL414420 Ki = 275.0 nM 6.56