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Assay Detail

CHEMBL772411

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

Binding
Binding affinity against RAS guanyl releasing protein using [3H]- PDBu as the labeled ligand
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

RAS guanyl-releasing protein 1 (CHEMBL3109)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structural basis of RasGRP binding to high-affinity PKC ligands.
Rong SB, Enyedy IJ, Qiao L, Zhao L, Ma D, Pearce LL, Lorenzo PS, Stone JC, Blumberg PM, Wang S, Kozikowski AP.
J Med Chem (2002) 45 : 853 -860
PubMed 11831896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.44 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285801 1 9.07
CHEMBL27266 INDOLACTUM 1 8.60
CHEMBL6453 1 8.21
CHEMBL7078 1 7.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285801 Ki = 0.85 nM 9.07
CHEMBL27266 INDOLACTUM Ki = 2.54 nM 8.60
CHEMBL6453 Ki = 6.15 nM 8.21
CHEMBL7078 Ki = 13.92 nM 7.86