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Assay Detail

CHEMBL948823

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

Binding
Inhibition of GST-tagged IGF1R (957-1367) expressed in baculovirus by time-resolved fluorescence assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Insulin-like growth factor 1 receptor (CHEMBL1957)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
Emmitte KA, Wilson BJ, Baum EW, Emerson HK, Kuntz KW, Nailor KE, Salovich JM, Smith SC, Cheung M, Gerding RM, Stevens KL, Uehling DE, Mook RA, Moorthy GS, Dickerson SH, Hassell AM, Leesnitzer MA, Shewchuk LM, Groy A, Rowand JL, Anderson K, Atkins CL, Yang J, Sabbatini P, Kumar R.
Bioorg Med Chem Lett (2009) 19 : 1004 -1008
PubMed 19101143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.25 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL448668 1 9.00
CHEMBL500198 1 9.00
CHEMBL447668 1 8.70
CHEMBL453438 1 8.70
CHEMBL506862 1 8.70
CHEMBL502652 1 8.70
CHEMBL502198 1 8.70
CHEMBL508627 1 8.70
CHEMBL449110 1 8.70
CHEMBL447639 1 8.52
CHEMBL500003 1 8.40
CHEMBL454796 1 8.40
CHEMBL507714 1 8.30
CHEMBL444031 1 8.15
CHEMBL448929 1 8.15
CHEMBL447450 1 8.00
CHEMBL466397 1 7.57
CHEMBL480544 1 7.55
CHEMBL504398 1 6.75
CHEMBL513227 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL448668 IC50 = 1.0 nM 9.00
CHEMBL500198 IC50 = 1.0 nM 9.00
CHEMBL447668 IC50 = 2.0 nM 8.70
CHEMBL453438 IC50 = 2.0 nM 8.70
CHEMBL506862 IC50 = 2.0 nM 8.70
CHEMBL502652 IC50 = 2.0 nM 8.70
CHEMBL502198 IC50 = 2.0 nM 8.70
CHEMBL508627 IC50 = 2.0 nM 8.70
CHEMBL449110 IC50 = 2.0 nM 8.70
CHEMBL447639 IC50 = 3.0 nM 8.52
CHEMBL500003 IC50 = 4.0 nM 8.40
CHEMBL454796 IC50 = 4.0 nM 8.40
CHEMBL507714 IC50 = 5.0 nM 8.30
CHEMBL444031 IC50 = 7.0 nM 8.15
CHEMBL448929 IC50 = 7.0 nM 8.15
CHEMBL447450 IC50 = 10.0 nM 8.00
CHEMBL466397 IC50 = 27.0 nM 7.57
CHEMBL480544 IC50 = 28.0 nM 7.55
CHEMBL504398 IC50 = 180.0 nM 6.75
CHEMBL513227 IC50 = 440.0 nM 6.36