colchicine [Ligand Id: 2367] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL107 (Gloperba, Colchicine, NSC-757, Colcrys, Mitigare)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
There should be some charts here, you may need to enable JavaScript!
  • Organic cation transporter 3/Solute carrier family 22 member 3 in Human [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • tubulin beta class I/Tubulin beta-5 chain in Human [ChEMBL: CHEMBL5444] [GtoPdb: 2640] [UniProtKB: P07437]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Tubulin polymerization-promoting protein in Bovine [ChEMBL: CHEMBL2366491] [UniProtKB: Q27957]
There should be some charts here, you may need to enable JavaScript!
  • glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
There should be some charts here, you may need to enable JavaScript!
  • glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
There should be some charts here, you may need to enable JavaScript!
  • bromodomain containing 4 in Human [GtoPdb: 1945] [UniProtKB: O60885]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Inhibition of human PIM1 measured after 5 mins by ELISA relative to control B 5.37 pIC50 4300 nM IC50 Eur J Med Chem (2017) 134: 357-365 [PMID:28431341]
Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake in OCT3-expressing HEK293 cells F 6.92 pKi 120 nM Ki Nat. Neurosci. (1998) 1: 349-351 [PMID:10196521]
tubulin beta class I/tubulin alpha 4a/tubulin beta 4B class IVb/tubulin beta 3 class III/tubulin beta 8 class VIII/tubulin alpha 1a/Tubulin in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095182] [GtoPdb: 264026392641275227532638] [UniProtKB: P04350P07437P0DPH7P68363P68366P68371Q13509Q13885Q3ZCM7Q6PEY2Q71U36Q9BQE3Q9BUF5Q9BVA1Q9H4B7]
ChEMBL Binding affinity to tubulin (unknown origin) assessed as dissociation constant by SPR analysis B 4.95 pKd 11300 nM Kd Eur J Med Chem (2019) 170: 73-86 [PMID:30878833]
ChEMBL Binding affinity to tubulin (unknown origin) by ITC method B 7.24 pKd 58 nM Kd Eur J Med Chem (2017) 141: 460-472 [PMID:29055869]
ChEMBL Displacement of [3H]-colchicine from biotin-labeled tubulin (unknown origin) after 2 hrs by scintillation proximity assay B 5.62 pKi 2400 nM Ki J. Med. Chem. (2013) 56: 8008-8018 [PMID:24106982]
ChEMBL Inhibition of brain tubulin (unknown origin) polymerization measured up to 15 to 30 mins B 5.11 pIC50 7800 nM IC50 J. Med. Chem. (2015) 58: 6678-6696 [PMID:26226379]
ChEMBL Inhibition of tubulin (unknown origin) polymerization by spectrophotometry B 5.27 pIC50 5400 nM IC50 Bioorg. Med. Chem. (2014) 22: 4917-4923 [PMID:25059503]
ChEMBL In vitro inhibition of tubulin polymerization. F 5.38 pIC50 4200 nM IC50 J. Med. Chem. (1993) 36: 1474-1479 [PMID:8496915]
ChEMBL Inhibition of tubulin polymerization F 5.48 pIC50 3300 nM IC50 J. Med. Chem. (2006) 49: 6656-6659 [PMID:17154496]
ChEMBL Inhibition of tubulin polymerization F 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2006) 49: 6412-6415 [PMID:17034147]
ChEMBL Inhibition of tubulin (unknown origin) polymerization incubated 15 mins prior to GTP addition by spectrophotometry B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2014) 57: 6531-6552 [PMID:25025991]
ChEMBL Inhibition of tubulin (unknown origin) assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric analysis B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2015) 58: 5789-5807 [PMID:26132075]
ChEMBL Inhibition of tubulin polymerization (unknown origin) incubated for 15 mins followed by GTP addition and measured for 20 mins by spectrophotometry B 5.49 pIC50 3200 nM IC50 Eur J Med Chem (2020) 185: 111828-111828 [PMID:31727471]
ChEMBL Inhibition of tubulin polymerization (unknown origin) preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric method B 5.49 pIC50 3200 nM IC50 Eur J Med Chem (2018) 152: 283-297 [PMID:29730191]
ChEMBL Inhibition of tubulin polymerization B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2004) 47: 6120-6123 [PMID:15566282]
ChEMBL Inhibition of tubulin polymerization B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2007) 50: 2865-2874 [PMID:17497841]
ChEMBL Inhibition of tubulin (unknown origin) polymerization preincubated for 15 mins by spectrophotometry B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2013) 56: 123-149 [PMID:23214452]
ChEMBL Inhibition of tubulin polymerization in presence of microtubule associated proteins after 30 mins B 5.54 pIC50 2900 nM IC50 J. Med. Chem. (2007) 50: 4548-4552 [PMID:17685504]
ChEMBL Inhibition of tubulin polymerization B 5.57 pIC50 2700 nM IC50 J. Med. Chem. (2006) 49: 2357-2360 [PMID:16570932]
ChEMBL Inhibition of tubulin polymerization (unknown origin) by DAPI staining-based fluorescence microscopy B 5.59 pIC50 2600 nM IC50 J. Med. Chem. (2014) 57: 6364-6382 [PMID:25061803]
ChEMBL Displacement of [3H]-colchicine from tubulin (unknown origin) preincubated with protein for 1 hr followed by [3H]-colchicine addition measured after 3 hrs by scintillation counting analysis B 5.66 pIC50 2210 nM IC50 J. Med. Chem. (2015) 58: 6549-6558 [PMID:26241032]
ChEMBL Inhibition of tubulin polymerization F 5.72 pIC50 1900 nM IC50 J. Med. Chem. (1993) 36: 1146-1156 [PMID:8387598]
ChEMBL Inhibition of microtubule polymerization F 5.77 pIC50 1700 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 2761-2764 [PMID:16504507]
ChEMBL Inhibition of Tubulin polymerization after 20 minutes of administration at 30 degree Centigrade F 5.82 pIC50 1500 nM IC50 J. Med. Chem. (1997) 40: 961-966 [PMID:9083485]
ChEMBL In vitro inhibition of mammalian tubulin polymerization by 50% B 5.82 pIC50 1500 nM IC50 J. Med. Chem. (1998) 41: 1956-1961 [PMID:9599244]
ChEMBL Inhibition of tubulin polymerization in human K562 cells B 5.85 pIC50 1400 nM IC50 Eur. J. Med. Chem. (2010) 45: 3354-3364 [PMID:20546980]
ChEMBL In vitro inhibitory activity against tubulin polymerization (10 uM) B 5.85 pIC50 1400 nM IC50 J. Med. Chem. (1998) 41: 2333-2338 [PMID:9632366]
ChEMBL Inhibition of tubulin polymerization (unknown origin) preincubated for 10 mins followed by GTP addition measured after 20 mins by Coomassie blue staining based SDS-PAGE analysis B 5.88 pIC50 1320 nM IC50 Eur J Med Chem (2017) 141: 460-472 [PMID:29055869]
ChEMBL Displacement of [3H]colchicine from biotinylated tubulin by scintillation proximity assay B 5.98 pIC50 1050 nM IC50 J. Med. Chem. (2007) 50: 6059-6066 [PMID:17973361]
ChEMBL Inhibition of [3H]colchicine binding to beta tubulin B 6.3 pIC50 500 nM IC50 J. Med. Chem. (2006) 49: 5769-5776 [PMID:16970401]
ChEMBL Inhibition of tubulin (unknown origin) polymerization preincubated for 45 mins followed by GTP addition measured after 2 hrs by fluorescence assay B 6.44 pIC50 360 nM IC50 Eur. J. Med. Chem. (2015) 93: 93-100 [PMID:25659770]
GtoPdb - - 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (2006) 16: 2761-4 [PMID:16504507]
Tubulin in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111464] [UniProtKB: Q6B856Q862F3]
ChEMBL Inhibition of bovine brain tubulin polymerization extent after 20 mins by turbidimetrically B 5.58 pIC50 2620 nM IC50 Eur. J. Med. Chem. (2015) 99: 125-137 [PMID:26070164]
ChEMBL Inhibition of bovine brain tubulin polymerization after 30 mins B 5.72 pIC50 1900 nM IC50 Bioorg. Med. Chem. (2015) 23: 4230-4236 [PMID:26160020]
Tubulin alpha chain in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3658] [UniProtKB: P02550]
ChEMBL Compound was evaluated for its ability to inhibit the binding of [3H]-colchicine to tubulin in competitive binding assay B 5.6 pKi 2500 nM Ki Bioorg. Med. Chem. Lett. (1991) 1: 471-476
ChEMBL Inhibition of tubulin polymerization interacting at the colchicine binding site. B 5.38 pIC50 4168.69 nM IC50 J. Med. Chem. (2000) 43: 167-176 [PMID:10649972]
ChEMBL Tested for 50 % inhibition of tubulin polymerization by turbidimetric assay B 5.72 pIC50 1900 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 581-584
ChEMBL The compound was evaluated in vitro for the mammalian brain tubulin polymerization using standard assay. F 5.82 pIC50 1500 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1257-1262
ChEMBL Inhibition of tubulin polymerization (ITP) B 6.1 pIC50 800 nM IC50 J. Med. Chem. (2001) 44: 3932-3936 [PMID:11689079]
tubulin beta class I/Tubulin beta-5 chain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5444] [GtoPdb: 2640] [UniProtKB: P07437]
ChEMBL Inhibition of tubulin beta polymerization in human Caco2 cells after 48 hrs by ELISA B 5.11 pIC50 7710 nM IC50 MedChemComm (2018) 9: 1511-1528
ChEMBL Inhibition of tubulin beta polymerization in human MCF7 cells after 18 to 24 hrs by ELISA based spectrophotometric analysis B 5.16 pIC50 6930 nM IC50 Bioorg Med Chem (2018) 26: 3474-3490 [PMID:29793751]
ChEMBL Inhibition of tubulin beta polymerization in human MCF7 cells after 48 hrs by ELISA B 5.34 pIC50 4590 nM IC50 MedChemComm (2018) 9: 1511-1528
GtoPdb - - 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (2006) 16: 2761-4 [PMID:16504507]
Tubulin beta chain in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3394] [UniProtKB: Q6B856]
ChEMBL Binding constant at colchicine site of bovine brain tubulin B 6.11 pKi 780 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 465-469 [PMID:11814821]
ChEMBL Compound was evaluated for in vitro inhibitory activity against polymerization of tubulin into microtubules isolated from bovine brain at 1 mg/mL tubulin concentration B 5.46 pIC50 3500 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 565-570
ChEMBL Inhibitory effect on the polymerization of purified bovine brain tubulin. F 5.62 pIC50 2400 nM IC50 J. Med. Chem. (1990) 33: 567-571 [PMID:2299625]
ChEMBL Inhibition of tubulin polymerization F 6.1 pIC50 800 nM IC50 J. Med. Chem. (1994) 37: 1126-1135 [PMID:8164254]
ChEMBL Inhibition of bovine tubulin polymerization F 6.1 pIC50 800 nM IC50 J. Med. Chem. (1997) 40: 2266-2275 [PMID:9216846]
Tubulin polymerization-promoting protein in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366491] [UniProtKB: Q27957]
ChEMBL Inhibition of Bos taurus (bovine) brain tubulin polymerization B 6.12 pEC50 750 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1393-1396 [PMID:11378362]
glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
GtoPdb - - 3.5 pIC50 324000 nM IC50
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
GtoPdb - - 4.2 pIC50 64000 nM IC50
bromodomain containing 4 in Human [GtoPdb: 1945] [UniProtKB: O60885]
GtoPdb - - 4.7 pKd 20000 nM Kd Angew Chem Int Ed Engl (2013) 52: 14055-9 [PMID:24272870]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]