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Assay Detail

CHEMBL4181452

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Functional
Antiproliferative activity against human NCI-H226 cells after 72 hrs by MTS assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H226
Confidence 1 — Organism
Curated By Intermediate

Target

NCI-H226 (CHEMBL614740)
Type CELL-LINE
Organism Homo sapiens

Publication

Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads.
Donnell AF, Zhang Y, Stang EM, Wei DD, Tebben AJ, Perez HL, Schroeder GM, Pan C, Rao C, Borzilleri RM, Vite GD, Gangwar S.
Bioorg Med Chem Lett (2017) 27 : 5267 -5271
PubMed 29102228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.69 10.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205723 1 10.62
CHEMBL4213013 1 10.33
CHEMBL4214485 1 9.93
CHEMBL4217429 1 9.45
CHEMBL4218141 1 9.18
CHEMBL4209576 1 9.00
CHEMBL4217945 1 8.97
CHEMBL4212187 1 8.80
CHEMBL4202522 1 8.09
CHEMBL4202586 1 8.06
CHEMBL4207470 1 7.92
CHEMBL279754 DSB-120 1 7.16
CHEMBL4210094 1 7.16
CHEMBL4205196 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205723 IC50 = 0.024 nM 10.62
CHEMBL4213013 IC50 = 0.047 nM 10.33
CHEMBL4214485 IC50 = 0.117 nM 9.93
CHEMBL4217429 IC50 = 0.355 nM 9.45
CHEMBL4218141 IC50 = 0.655 nM 9.18
CHEMBL4209576 IC50 = 0.993 nM 9.00
CHEMBL4217945 IC50 = 1.07 nM 8.97
CHEMBL4212187 IC50 = 1.6 nM 8.80
CHEMBL4202522 IC50 = 8.1 nM 8.09
CHEMBL4202586 IC50 = 8.7 nM 8.06
CHEMBL4207470 IC50 = 12.0 nM 7.92
CHEMBL279754 DSB-120 IC50 = 70.0 nM 7.16
CHEMBL4210094 IC50 = 69.0 nM 7.16
CHEMBL4205196 IC50 = 109.0 nM 6.96