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Assay Detail

CHEMBL616773

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

Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
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 (CHEMBL3459)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Central serotonin receptors as targets for drug research.
Glennon RA.
J Med Chem (1987) 30 : 1 -12
PubMed 3543362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.38 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18785 RU-24969 1 8.40
CHEMBL18840 1 8.30
CHEMBL19215 METERGOLINE 2.0 1 7.60
CHEMBL39 SEROTONIN 3.0 1 7.60
CHEMBL274866 1 7.52
CHEMBL277362 1 7.35
CHEMBL452861 LEVOPROPRANOLOL 2.0 1 7.30
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 7.12
CHEMBL500 PINDOLOL 4.0 1 7.10
CHEMBL7257 MEBUFOTENIN 2.0 1 7.05
CHEMBL18772 QUIPAZINE 2.0 1 6.50
CHEMBL8165 5-METHOXYTRYPTAMINE 2 6.40
CHEMBL416526 BUFOTENINE 1 6.04
CHEMBL275854 1 6.00
CHEMBL18786 CINANSERIN 2.0 1 6.00
CHEMBL18855 1 5.98
CHEMBL51 KETANSERIN 3.0 1 5.72
CHEMBL6437 MIANSERIN 4.0 1 5.33
CHEMBL267930 SPIPERONE 2.0 1 5.32
CHEMBL19264 1 5.23
CHEMBL18331 PIRENPERONE 2.0 1 5.18
CHEMBL6640 TRYPTAMINE 1 4.99
CHEMBL12314 MESULERGINE 2.0 1 4.89
CHEMBL56 8-OH-DPAT 1 4.20
CHEMBL134519 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18785 RU-24969 Ki = 4.0 nM 8.40
CHEMBL18840 Ki = 5.0 nM 8.30
CHEMBL39 SEROTONIN Ki = 25.0 nM 7.60
CHEMBL19215 METERGOLINE Ki = 25.0 nM 7.60
CHEMBL274866 Ki = 30.0 nM 7.52
CHEMBL277362 Ki = 45.0 nM 7.35
CHEMBL452861 LEVOPROPRANOLOL Ki = 50.0 nM 7.30
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 75.0 nM 7.12
CHEMBL500 PINDOLOL Ki = 80.0 nM 7.10
CHEMBL7257 MEBUFOTENIN Ki = 90.0 nM 7.05
CHEMBL18772 QUIPAZINE Ki = 320.0 nM 6.50
CHEMBL8165 5-METHOXYTRYPTAMINE Ki = 400.0 nM 6.40
CHEMBL8165 5-METHOXYTRYPTAMINE Ki = 400.0 nM 6.40
CHEMBL416526 BUFOTENINE Ki = 910.0 nM 6.04
CHEMBL275854 Ki = 1000.0 nM 6.00
CHEMBL18786 CINANSERIN Ki = 1000.0 nM 6.00
CHEMBL18855 Ki = 1050.0 nM 5.98
CHEMBL51 KETANSERIN Ki = 1900.0 nM 5.72
CHEMBL6437 MIANSERIN Ki = 4700.0 nM 5.33
CHEMBL267930 SPIPERONE Ki = 4800.0 nM 5.32
CHEMBL19264 Ki = 5890.0 nM 5.23
CHEMBL18331 PIRENPERONE Ki = 6600.0 nM 5.18
CHEMBL6640 TRYPTAMINE Ki = 10200.0 nM 4.99
CHEMBL12314 MESULERGINE Ki = 13000.0 nM 4.89
CHEMBL56 8-OH-DPAT Ki = 63000.0 nM 4.20
CHEMBL134519 Ki - nM -