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Assay Detail

CHEMBL965237

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

Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
Choi SK, Green D, Ho A, Klein U, Marquess D, Taylor R, Turner SD.
J Med Chem (2008) 51 : 3609 -3616
PubMed 18507369 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 8.17 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374973 1 10.00
CHEMBL144030 1 10.00
CHEMBL502138 1 9.30
CHEMBL500284 1 9.24
CHEMBL158941 1 9.19
CHEMBL31217 1 9.12
CHEMBL444404 1 9.12
CHEMBL452387 1 9.10
CHEMBL500488 1 9.09
CHEMBL39 SEROTONIN 3.0 1 8.96
CHEMBL446745 1 8.89
CHEMBL448902 1 8.89
CHEMBL128 SUMATRIPTAN 4.0 1 8.04
CHEMBL489453 1 7.80
CHEMBL448555 1 7.75
CHEMBL501645 1 7.50
CHEMBL500230 1 7.42
CHEMBL503468 1 7.10
CHEMBL101690 1 7.08
CHEMBL500737 1 7.00
CHEMBL450852 1 6.99
CHEMBL505750 1 6.90
CHEMBL509314 1 6.90
CHEMBL521235 1 6.45
CHEMBL451394 1 6.34
CHEMBL510280 1 -
CHEMBL505954 1 -
CHEMBL453939 1 -
CHEMBL483497 1 -
CHEMBL519492 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374973 Ki = 0.1 nM 10.00
CHEMBL144030 Ki = 0.1 nM 10.00
CHEMBL502138 Ki = 0.5 nM 9.30
CHEMBL500284 Ki = 0.58 nM 9.24
CHEMBL158941 Ki = 0.64 nM 9.19
CHEMBL31217 Ki = 0.76 nM 9.12
CHEMBL444404 Ki = 0.76 nM 9.12
CHEMBL452387 Ki = 0.79 nM 9.10
CHEMBL500488 Ki = 0.81 nM 9.09
CHEMBL39 SEROTONIN Ki = 1.1 nM 8.96
CHEMBL446745 Ki = 1.3 nM 8.89
CHEMBL448902 Ki = 1.3 nM 8.89
CHEMBL128 SUMATRIPTAN Ki = 9.1 nM 8.04
CHEMBL489453 Ki = 16.0 nM 7.80
CHEMBL448555 Ki = 18.0 nM 7.75
CHEMBL501645 Ki = 32.0 nM 7.50
CHEMBL500230 Ki = 38.0 nM 7.42
CHEMBL503468 Ki = 79.0 nM 7.10
CHEMBL101690 Ki = 83.0 nM 7.08
CHEMBL500737 Ki = 100.0 nM 7.00
CHEMBL450852 Ki = 103.0 nM 6.99
CHEMBL505750 Ki = 126.0 nM 6.90
CHEMBL509314 Ki = 126.0 nM 6.90
CHEMBL521235 Ki = 353.0 nM 6.45
CHEMBL451394 Ki = 453.0 nM 6.34
CHEMBL500749 Ki > 10000.0 nM -
CHEMBL454766 Ki > 1000.0 nM -
CHEMBL487313 Ki > 1000.0 nM -
CHEMBL488951 Ki > 1000.0 nM -
CHEMBL488125 Ki > 1000.0 nM -
CHEMBL483498 Ki > 1000.0 nM -
CHEMBL519492 Ki > 1000.0 nM -
CHEMBL483497 Ki > 1000.0 nM -
CHEMBL453939 Ki > 1000.0 nM -
CHEMBL505954 Ki > 10000.0 nM -
CHEMBL510280 Ki > 10000.0 nM -