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Assay Detail

CHEMBL839747

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

Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1B (CHEMBL1898)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
Ward SE, Harrington FP, Gordon LJ, Hopley SC, Scott CM, Watson JM.
J Med Chem (2005) 48 : 3478 -3480
PubMed 15887956 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.69 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183460 1 8.00
CHEMBL190298 1 7.20
CHEMBL191605 1 7.10
CHEMBL192176 1 7.00
CHEMBL2113061 1 6.80
CHEMBL364495 1 6.70
CHEMBL425190 1 6.70
CHEMBL191921 1 6.60
CHEMBL191895 1 6.60
CHEMBL192536 1 6.60
CHEMBL193268 1 6.50
CHEMBL362992 1 6.50
CHEMBL365810 1 6.40
CHEMBL190190 1 6.40
CHEMBL363413 1 6.20
CHEMBL191980 1 5.70
CHEMBL191619 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183460 Ki = 10.0 nM 8.00
CHEMBL190298 Ki = 63.1 nM 7.20
CHEMBL191605 Ki = 79.43 nM 7.10
CHEMBL192176 Ki = 100.0 nM 7.00
CHEMBL2113061 Ki = 158.49 nM 6.80
CHEMBL364495 Ki = 199.53 nM 6.70
CHEMBL425190 Ki = 199.53 nM 6.70
CHEMBL191921 Ki = 251.19 nM 6.60
CHEMBL191895 Ki = 251.19 nM 6.60
CHEMBL192536 Ki = 251.19 nM 6.60
CHEMBL193268 Ki = 316.23 nM 6.50
CHEMBL362992 Ki = 316.23 nM 6.50
CHEMBL365810 Ki = 398.11 nM 6.40
CHEMBL190190 Ki = 398.11 nM 6.40
CHEMBL363413 Ki = 630.96 nM 6.20
CHEMBL191980 Ki = 1995.26 nM 5.70
CHEMBL191619 Ki < 10000.0 nM -