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Assay Detail

CHEMBL663558

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

Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Corticotropin-releasing factor receptor 1 (CHEMBL1800)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rapid microscale synthesis, a new method for lead optimization using robotics and solution phase chemistry: application to the synthesis and optimization of corticotropin-releasing factor1 receptor antagonists.
Whitten JP, Xie YF, Erickson PE, Webb TR, De Souza EB, Grigoriadis DE, McCarthy JR.
J Med Chem (1996) 39 : 4354 -4357
PubMed 8893828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 5.95 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL306618 1 7.24
CHEMBL77391 1 6.94
CHEMBL308544 1 6.89
CHEMBL419636 1 6.31
CHEMBL307419 1 6.31
CHEMBL305671 1 5.98
CHEMBL78035 1 5.98
CHEMBL307871 1 5.83
CHEMBL78271 1 5.77
CHEMBL137434 1 5.77
CHEMBL77527 1 5.68
CHEMBL136519 1 5.24
CHEMBL136828 1 5.10
CHEMBL343073 1 4.26
CHEMBL343704 1 -
CHEMBL343343 1 -
CHEMBL137122 1 -
CHEMBL137666 1 -
CHEMBL137610 1 -
CHEMBL78203 1 -
CHEMBL337096 1 -
CHEMBL138597 1 -
CHEMBL138124 1 -
CHEMBL343958 1 -
CHEMBL136596 1 -
CHEMBL135615 1 -
CHEMBL137291 1 -
CHEMBL137123 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL306618 Ki = 57.0 nM 7.24
CHEMBL77391 Ki = 115.0 nM 6.94
CHEMBL308544 Ki = 130.0 nM 6.89
CHEMBL419636 Ki = 490.0 nM 6.31
CHEMBL307419 Ki = 490.0 nM 6.31
CHEMBL305671 Ki = 1050.0 nM 5.98
CHEMBL78035 Ki = 1050.0 nM 5.98
CHEMBL307871 Ki = 1470.0 nM 5.83
CHEMBL78271 Ki = 1690.0 nM 5.77
CHEMBL137434 Ki = 1700.0 nM 5.77
CHEMBL77527 Ki = 2100.0 nM 5.68
CHEMBL136519 Ki = 5700.0 nM 5.24
CHEMBL136828 Ki = 8000.0 nM 5.10
CHEMBL343073 Ki = 55000.0 nM 4.26
CHEMBL343704 Ki > 10000.0 nM -
CHEMBL343343 Ki > 10000.0 nM -
CHEMBL137122 Ki > 10000.0 nM -
CHEMBL137666 Ki > 10000.0 nM -
CHEMBL137610 Ki > 10000.0 nM -
CHEMBL78203 Ki > 10000.0 nM -
CHEMBL337096 Ki > 10000.0 nM -
CHEMBL138597 Ki > 10000.0 nM -
CHEMBL138124 Ki > 10000.0 nM -
CHEMBL343958 Ki > 10000.0 nM -
CHEMBL136596 Ki > 10000.0 nM -
CHEMBL135615 Ki > 10000.0 nM -
CHEMBL137291 Ki > 10000.0 nM -
CHEMBL137123 Ki > 10000.0 nM -