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Assay Detail

CHEMBL4617610

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

Binding
Inhibition of human CLR/RAMP1
19
Total Activities
19
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Blocking the CGRP Pathway for Acute and Preventive Treatment of Migraine: The Evolution of Success.
Dubowchik GM, Conway CM, Xin AW.
J Med Chem (2020) 63 : 6600 -6623
PubMed 32058712 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.07 10.52
Ki 9 9.27 10.70
Kb 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4638635 1 10.70
CHEMBL207197 OLCEGEPANT 2.0 1 10.52
CHEMBL4635331 HTL-0022562 1.0 1 10.40
CHEMBL4633407 1 9.96
CHEMBL4644508 1 9.85
CHEMBL4637301 1 9.82
CHEMBL4639133 1 9.70
CHEMBL4649671 1 9.60
CHEMBL3334624 BI-44370 2.0 1 9.52
CHEMBL236593 TELCAGEPANT 3.0 1 9.11
CHEMBL4641806 1 8.33
CHEMBL3334623 1 7.36
CHEMBL4645875 1 6.60
CHEMBL4634626 1 6.00
CHEMBL4634646 1 5.32
CHEMBL196582 1 4.77
CHEMBL4643140 1 -
CHEMBL4640176 1 -
CHEMBL4649325 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4638635 Ki = 0.02 nM 10.70
CHEMBL207197 OLCEGEPANT IC50 = 0.03 nM 10.52
CHEMBL4635331 HTL-0022562 Ki = 0.04 nM 10.40
CHEMBL4633407 Ki = 0.11 nM 9.96
CHEMBL4644508 IC50 = 0.14 nM 9.85
CHEMBL4637301 Ki = 0.15 nM 9.82
CHEMBL4639133 IC50 = 0.2 nM 9.70
CHEMBL4649671 Ki = 0.25 nM 9.60
CHEMBL3334624 BI-44370 IC50 = 0.3 nM 9.52
CHEMBL236593 TELCAGEPANT Ki = 0.77 nM 9.11
CHEMBL4641806 IC50 = 4.7 nM 8.33
CHEMBL3334623 IC50 = 44.0 nM 7.36
CHEMBL4645875 IC50 = 250.0 nM 6.60
CHEMBL4634626 IC50 = 1000.0 nM 6.00
CHEMBL4634646 Ki = 4800.0 nM 5.32
CHEMBL196582 IC50 = 17000.0 nM 4.77
CHEMBL4643140 Ki = 0.004 nM -
CHEMBL4640176 Kb = 0.31 nM -
CHEMBL4649325 Ki = 0.007 nM -