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Assay Detail

CHEMBL664986

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

Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebellum
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Corticotropin-releasing factor receptor 1 (CHEMBL4649)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: the development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor.
Hsin LW, Webster EL, Chrousos GP, Gold PW, Eckelman WC, Contoreggi C, Rice KC.
Bioorg Med Chem Lett (2000) 10 : 707 -710
PubMed 10782669 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.38 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434882 1 9.04
CHEMBL164206 1 8.64
CHEMBL296641 ANTALARMIN 1 8.60
CHEMBL348967 1 8.46
CHEMBL163618 1 8.00
CHEMBL164042 1 7.52
CHEMBL159575 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434882 Ki = 0.91 nM 9.04
CHEMBL164206 Ki = 2.3 nM 8.64
CHEMBL296641 ANTALARMIN Ki = 2.5 nM 8.60
CHEMBL348967 Ki = 3.5 nM 8.46
CHEMBL163618 Ki = 10.0 nM 8.00
CHEMBL164042 Ki = 30.0 nM 7.52
CHEMBL159575 Ki > 1000.0 nM -